TMPRSS2

Summary

TMPRSS2 (transmembrane serine protease 2, HGNC:11876) is a protein-coding gene on chromosome 21q22.3, encoding Transmembrane protease serine 2 (O15393). Plasma membrane-anchored serine protease that cleaves at arginine residues.

This gene encodes a protein that belongs to the serine protease family. The encoded protein contains a type II transmembrane domain, a receptor class A domain, a scavenger receptor cysteine-rich domain and a protease domain. Serine proteases are known to be involved in many physiological and pathological processes. This gene was demonstrated to be up-regulated by androgenic hormones in prostate cancer cells and down-regulated in androgen-independent prostate cancer tissue. The protease domain of this protein is thought to be cleaved and secreted into cell media after autocleavage. This protein also facilitates entry of viruses into host cells by proteolytically cleaving and activating viral envelope glycoproteins. Viruses found to use this protein for cell entry include Influenza virus and the human coronaviruses HCoV-229E, MERS-CoV, SARS-CoV and SARS-CoV-2 (COVID-19 virus). Alternatively spliced transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 7113 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 35 total — 1 pathogenic
• GTEx eGene: eQTL in 10 tissues, sQTL in 0 (q < 0.05)
• ChEMBL bioactivity: 9 clinical-phase molecules tested; no curated mechanism-of-action drug
• Cancer driver (intOGen): activating (oncogene-like) across 1 cancer types (inferred from mutation patterns)
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.99 (unconstrained)
• MANE Select transcript: NM_005656
• Interaction hub: 2,385 STRING partners (top 5% of genes corpus-wide)

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11876
Approved symbol	TMPRSS2
Name	transmembrane serine protease 2
Location	21q22.3
Locus type	gene with protein product
Status	Approved
Aliases	PRSS10
Ensembl gene	ENSG00000184012
Ensembl biotype	protein_coding
OMIM	602060
Entrez	7113

Gene structure

Transcript identifiers

Ensembl transcripts: 48 — 35 protein_coding, 9 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined, 2 retained_intron

MANE Select: ENST00000332149

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 4, TSL 3: 1, TSL 5: 2

ENST00000332149, ENST00000398585, ENST00000424093, ENST00000454499, ENST00000455813, ENST00000458356, ENST00000463138, ENST00000469395, ENST00000489201, ENST00000676973, ENST00000677680, ENST00000678171, ENST00000678348, ENST00000678617, ENST00000678743, ENST00000678959, ENST00000679016, ENST00000679054, ENST00000679181, ENST00000679263, ENST00000864262, ENST00000864263, ENST00000864264, ENST00000864265, ENST00000864266, ENST00000864267, ENST00000864268, ENST00000864269, ENST00000864270, ENST00000864271, ENST00000864272, ENST00000864273, ENST00000864274, ENST00000864275, ENST00000864276, ENST00000864277, ENST00000966230, ENST00000966231, ENST00000966232, ENST00000966233, ENST00001007444, ENST00001007445, ENST00001007446, ENST00001048272, ENST00001048274, ENST00001063017, ENST00001063018, ENST00001063019

RefSeq mRNA: 3 — MANE Select: NM_005656 NM_001135099, NM_001382720, NM_005656

CCDS: CCDS33564, CCDS54486, CCDS93100

Canonical transcript exons

ENST00000332149 — 14 exons

Exon	Start	End
ENSE00001291248	41473325	41473496
ENSE00001296629	41508081	41508158
ENSE00001296879	41479172	41479282
ENSE00001308618	41488394	41488513
ENSE00001309041	41470648	41470743
ENSE00001310536	41471806	41471981
ENSE00001319118	41476577	41476620
ENSE00001324661	41468396	41468538
ENSE00001328752	41480476	41480602
ENSE00001919654	41464305	41466153
ENSE00003500399	41489507	41489593
ENSE00003502036	41498119	41498189
ENSE00003786558	41467734	41467886
ENSE00003788834	41494356	41494578

Expression profiles

Bgee: expression breadth ubiquitous, 198 present calls, max score 98.78.

FANTOM5 (CAGE): breadth broad, TPM avg 3.1010 / max 241.3942, expressed in 362 samples.

Highest expression (Bgee): mucosa of transverse colon, mucosa of sigmoid colon, colonic mucosa, body of pancreas, rectum.

Genetic regulation across tissues (GTEx eQTL / sQTL)

TMPRSS2 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 10 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

10 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Testis	eqtl	2.5e-21	+0.55	21:41553100:A:G
Prostate	eqtl	1.0e-14	-0.33	21:41520129:G:A
Lung	eqtl	4.9e-10	+0.14	21:41485641:C:T
Skin Sun Exposed Lower leg	eqtl	3.5e-04	-0.10	21:41506684:C:T
Pituitary	eqtl	3.3e-03	+0.28	21:41549662:G:A
Brain Hypothalamus	eqtl	6.4e-03	+0.41	21:41493224:T:C
Thyroid	eqtl	1.2e-02	-0.10	21:41486054:G:A
Small Intestine Terminal Ileum	eqtl	2.5e-02	+0.29	21:41943370:A:T
Minor Salivary Gland	eqtl	3.4e-02	+1.26	21:40825106:G:GT
Skin Not Sun Exposed Suprapubic	eqtl	4.8e-02	-0.08	21:41878606:C:T

FANTOM5 promoters

3 alternative TSS:

Promoter ID	TPM avg	Samples expressed
190562	2.6714	327
190561	0.4240	238
190563	0.0055	2

Top tissues by expression

showing 100 of 289 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
mucosa of transverse colon	UBERON:0004991	98.78	gold quality
mucosa of sigmoid colon	UBERON:0004993	98.19	gold quality
colonic mucosa	UBERON:0000317	98.07	gold quality
body of pancreas	UBERON:0001150	97.91	gold quality
rectum	UBERON:0001052	97.55	gold quality
esophagus squamous epithelium	UBERON:0006920	95.51	gold quality
prostate gland	UBERON:0002367	94.95	gold quality
metanephros cortex	UBERON:0010533	94.70	gold quality
lower esophagus mucosa	UBERON:0035834	94.45	gold quality
parotid gland	UBERON:0001831	94.33	gold quality
epithelium of esophagus	UBERON:0001976	93.93	gold quality
duodenum	UBERON:0002114	93.75	gold quality
ileal mucosa	UBERON:0000331	93.61	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	93.04	gold quality
pancreas	UBERON:0001264	92.53	gold quality
pylorus	UBERON:0001166	92.26	gold quality
upper lobe of left lung	UBERON:0008952	91.97	gold quality
saliva-secreting gland	UBERON:0001044	91.75	gold quality
upper lobe of lung	UBERON:0008948	91.73	gold quality
cardia of stomach	UBERON:0001162	91.26	gold quality
gall bladder	UBERON:0002110	91.23	gold quality
minor salivary gland	UBERON:0001830	91.13	gold quality
transverse colon	UBERON:0001157	90.54	gold quality
stomach	UBERON:0000945	90.23	gold quality
adult mammalian kidney	UBERON:0000082	90.00	gold quality
body of stomach	UBERON:0001161	89.97	gold quality
type B pancreatic cell	CL:0000169	89.92	gold quality
small intestine Peyer’s patch	UBERON:0003454	89.92	gold quality
right lung	UBERON:0002167	89.69	gold quality
esophagus mucosa	UBERON:0002469	89.46	gold quality
mouth mucosa	UBERON:0003729	89.37	gold quality
lower lobe of lung	UBERON:0008949	89.21	gold quality
small intestine	UBERON:0002108	89.20	gold quality
jejunal mucosa	UBERON:0000399	88.83	gold quality
nasal cavity epithelium	UBERON:0005384	88.52	gold quality
nasal cavity mucosa	UBERON:0001826	87.88	gold quality
right lobe of liver	UBERON:0001114	87.86	gold quality
mucosa of paranasal sinus	UBERON:0005030	87.84	gold quality
squamous epithelium	UBERON:0006914	87.58	gold quality
lung	UBERON:0002048	87.49	gold quality
male germ cell	CL:0000015	87.07	gold quality
sperm	CL:0000019	86.99	gold quality
left lobe of thyroid gland	UBERON:0001120	86.92	gold quality
bronchial epithelial cell	CL:0002328	86.44	gold quality
olfactory bulb	UBERON:0002264	86.32	gold quality
right lobe of thyroid gland	UBERON:0001119	86.27	gold quality
epithelium of bronchus	UBERON:0002031	86.11	gold quality
epithelium of nasopharynx	UBERON:0001951	85.93	gold quality
bronchus	UBERON:0002185	85.76	gold quality
islet of Langerhans	UBERON:0000006	85.49	gold quality
renal medulla	UBERON:0000362	85.48	gold quality
mucosa of stomach	UBERON:0001199	85.45	gold quality
palpebral conjunctiva	UBERON:0001812	85.32	gold quality
amniotic fluid	UBERON:0000173	85.31	gold quality
triceps brachii	UBERON:0001509	85.20	gold quality
thyroid gland	UBERON:0002046	85.17	gold quality
kidney	UBERON:0002113	85.07	gold quality
gluteal muscle	UBERON:0002000	84.84	gold quality
liver	UBERON:0002107	84.13	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	84.04	gold quality
right uterine tube	UBERON:0001302	83.80	gold quality
fundus of stomach	UBERON:0001160	83.40	gold quality
intestine	UBERON:0000160	83.20	gold quality
colonic epithelium	UBERON:0000397	82.96	gold quality
tonsil	UBERON:0002372	82.87	gold quality
vermiform appendix	UBERON:0001154	82.81	gold quality
jejunum	UBERON:0002115	82.67	gold quality
caecum	UBERON:0001153	82.32	gold quality
buccal mucosa cell	CL:0002336	82.28	gold quality
oral cavity	UBERON:0000167	82.08	gold quality
tongue squamous epithelium	UBERON:0006919	81.29	gold quality
large intestine	UBERON:0000059	81.18	gold quality
colon	UBERON:0001155	80.48	gold quality
epithelial cell of pancreas	CL:0000083	80.13	silver quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	79.55	gold quality
gingival epithelium	UBERON:0001949	79.35	silver quality
gingiva	UBERON:0001828	79.10	gold quality
urinary bladder	UBERON:0001255	79.06	gold quality
mammary duct	UBERON:0001765	78.77	gold quality
oviduct epithelium	UBERON:0004804	78.64	silver quality
urethra	UBERON:0000057	78.13	gold quality
upper arm skin	UBERON:0004263	78.00	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.97	gold quality
epithelium of mammary gland	UBERON:0003244	77.72	silver quality
trachea	UBERON:0003126	77.66	gold quality
mucosa of urinary bladder	UBERON:0001259	77.65	silver quality
vastus lateralis	UBERON:0001379	77.65	gold quality
pancreatic ductal cell	CL:0002079	77.59	silver quality
cortex of kidney	UBERON:0001225	77.41	gold quality
skin of leg	UBERON:0001511	77.03	gold quality
superior surface of tongue	UBERON:0007371	76.63	gold quality
metanephros	UBERON:0000081	75.93	gold quality
periodontal ligament	UBERON:0008266	75.79	gold quality
mammary gland	UBERON:0001911	75.76	gold quality
thoracic mammary gland	UBERON:0005200	75.76	gold quality
pharyngeal mucosa	UBERON:0000355	75.75	gold quality
quadriceps femoris	UBERON:0001377	75.49	gold quality
tongue	UBERON:0001723	75.21	silver quality
biceps brachii	UBERON:0001507	75.18	gold quality
fallopian tube	UBERON:0003889	74.87	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-MTAB-10662	yes	190.68
E-CURD-119	yes	32.91
E-ANND-3	yes	23.12

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 71 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Prostate	tissue	263.4	medium
Stomach 1	tissue	138.0	medium
Colon	tissue	96.6	medium
Small intestine	tissue	84.3	low
Pancreas	tissue	81.4	medium
Duodenum	tissue	73.9	low
Rectum	tissue	73.2	high
Salivary gland	tissue	71.8	low
Lung	tissue	37.6	low
Urinary bladder	tissue	33.2	not detected
Liver	tissue	31.3	not detected
Kidney	tissue	30.2	high
Esophagus	tissue	23.3	not detected
Gallbladder	tissue	22.6	not detected
Breast	tissue	18.7	not detected
Appendix	tissue	13.1	low
Fallopian tube	tissue	10.1	not detected
Tonsil	tissue	9.6	not detected
Choroid plexus	tissue	8.2
Thyroid gland	tissue	7.4	not detected
Seminal vesicle	tissue	7.3	low
Vagina	tissue	7.1	not detected
Cervix	tissue	4.7	not detected
Parathyroid gland	tissue	3.7	medium
Smooth muscle	tissue	3.1	not detected
Epididymis	tissue	2.6	medium
Nucleus accumbens	tissue	2.4
Postcentral gyrus	tissue	2.1
Hippocampus	tissue	2.0	not detected
Locus coeruleus	tissue	1.9
Testis	tissue	1.4	not detected
Pituitary gland	tissue	1.3
Basal ganglia	tissue	1.1	not detected
Olfactory bulb	tissue	1.0
Endometrium 1	tissue	0.9	not detected
Putamen	tissue	0.7
Thymus	tissue	0.7
Ventral forebrain	tissue	0.7
Septum	tissue	0.7
Adipose tissue	tissue	0.6	not detected
Skin 1	tissue	0.4	not detected
Cerebral cortex	tissue	0.4	not detected
Motor cortex	tissue	0.4
Hypothalamus	tissue	0.4
Hippocampal formation	tissue	0.4
Somatosensory cortex	tissue	0.4
Temporal cortex	tissue	0.4
Occipital cortex	tissue	0.4
Prefrontal cortex	tissue	0.3
Amygdala	tissue	0.3
Entorhinal cortex	tissue	0.3
Retrosplenial and cingulate cortex	tissue	0.3
Periaqueductal gray	tissue	0.3
Insular cortex	tissue	0.3
Lymph node	tissue	0.2	not detected
Retina	tissue	0.2
Pons	tissue	0.2
Ovary	tissue	0.2	not detected
Thalamus	tissue	0.2
Superior colliculi	tissue	0.2

Brain sub-regions (HPA Brain Atlas): detected in 187; highest nTPM — Temporal white matter (2.6), Nucleus tractus solitarii (2.5), Olfactory area (2.5), Parieto-temporal junction (white matter) (2.5), Basal amygdala (2.4).

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets:

Target	Regulation
HGF	Activation

Upstream regulators (CollecTRI, top): AR, ERG, ESR1, ESR2, NCOA3, NKX3-1, VDR

miRNA regulators (miRDB)

Targeting TMPRSS2 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 63 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4500	99.99	72.72	2367
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-5696	99.98	72.36	4487
HSA-LET-7D-5P	99.96	71.76	1632
HSA-MIR-4458	99.96	71.64	1650
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-6845-3P	99.94	66.88	1439
HSA-MIR-7162-3P	99.89	68.16	1682
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-202-3P	99.84	71.41	1290
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-4802-3P	99.72	70.13	1273
HSA-MIR-1208	99.70	68.28	1533
HSA-MIR-4729	99.69	72.18	4233
HSA-MIR-646	99.68	67.84	1645
HSA-MIR-651-5P	99.64	68.49	1104
HSA-MIR-3679-3P	99.64	69.88	1599
HSA-MIR-6861-3P	99.60	68.46	444
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-4688	99.48	64.68	828
HSA-MIR-6743-5P	99.48	63.60	721

Functional genomics

gnomAD constraint: pLI 2.59e-15, LOEUF 0.991, missense Z -0.024 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000332149 — one region, missense o/e 1.04.

Literature-anchored findings (GeneRIF, showing 40)

• present study describes how TMPRSS2 may contribute to prostate tumour metastasis via the activation of PAR-2 (PMID:15537383)
• Data show the presence of the TMPRSS2/ERG gene fusion is common in prostate adenocarcinoma. (PMID:16575875)
• Dysregulation of ETS family members through fusions with TMRPSS2 may be an initiating event in prostate cancer development. (PMID:16585160)
• genomic microdeletion of chromosome 21 is associated with rearrangement, as shown by FISH analysis of TMPRSS2/ERG fusions in prostate cancer (PMID:16820092)
• TMPRSS2 and HAT are candidates for proteolytic activation of influenza viruses in vivo (PMID:16973594)
• demonstrate for the first time that the TMPRSS2-ERG fusion gene can be detected in a proportion of HGPIN lesions and that this molecular rearrangement is an early event that may precede chromosome-level alterations in prostate carcinogenesis (PMID:17032499)
• Gene is deleted in gastric and colorectal cancers. (PMID:17367471)
• findings show that the TMPRSS2-ERG fusion is common in prostate cancer and that the related TMPRSS2-ETV1 fusion is very rare; frequency of ERG-fusions in the present study is somewhat lower than previously observed (PMID:17390040)
• TMPRSS2:ERG prostate cancer gene fusion may lead to haploinsufficiency or additional fusion events. (PMID:17584912)
• TMPRSS2-ERV1 fusion protein was found in 1/82 prostate neoplasms. TMPRSS2-ERG fusion protein was found in 35/82 prostate neoplasms. (PMID:17632455)
• presence/absence of Alu family consensus sequence in the introns of TMPRSS2 and ERG correlates with the presence/absence of fusion transcripts and indicates consensus sequence may be involved in prostate cancer (PMID:17654723)
• Heterogeneity of TMPRSS2 gene rearrangements in multifocal prostate adenocarcinoma. (PMID:17804708)
• Frequent presence of the TMPRSS2-ERG in index tumors suggests critical roles of ERG alterations in the onset and progression of a large subset of prostate cancer. (PMID:18065961)
• A TMPRSS2:ETV5 gene fusion was identified in prostate cancer. (PMID:18172298)
• further study is required to address association between TMPRSS2:ERG fusion and prostate cancer metastasis, detection of genomic truncation of the ERG gene could be useful for monitoring appearance of CTC and potential for prostate cancer metastasis (PMID:18385909)
• Detection of ETS fusion gene by RT-PCR is feasible on formalin-fixed and paraffin-embedded samples. (PMID:18474293)
• TMPRSS2-ERG with interstitial deletion is an aggressive and, in this study, uniformly lethal molecular subtype of prostate cancer associated with androgen-independent disease (PMID:18483239)
• the detection of isolated TMPRSS2-ERG fusion high-grade prostatic intraepithelial neoplasia would improve the positive predictive value of finding TMPRSS2-ERG fusion prostate cancer in subsequent biopsies. (PMID:18519767)
• The TMPRSS2:ERG rearrangement can be found in about one third of prostate cancers. A subgroup of prostate cancer patients with a good prognosis may be identified by the rearrangement (PMID:18519769)
• Efficient multiplication of metapneumovirus in Vero cells expressing TMPRSS2 is reported. (PMID:18562527)
• Information of TMPRSS2:ERG fusion status improved prognostification of the multigene model. (PMID:18583469)
• analysis of the TMPRSS2-ERG splice variants in prostate cancer (PMID:18676740)
• TMPRSS2-ERG gene fusion has a role in prostate cancer characteristics and outcomes (PMID:18694509)
• TMPRSS2/ERG fusion isoforms have variable biological activities promoting tumor initiation and progression. (PMID:18922926)
• TMPRSS2-ERG fusion is frequently observed in Gleason pattern 3 prostate cancer in a Canadian cohort. (PMID:19029822)
• study detected the TMPRSS2-ERG fusion in 44 (59%) familial prostate cancer patients; findings revealed several loci located on chromosomes #9, #18, and X that were suggestive of linkage to the TMPRSS2-ERG fusion-positive prostate cancer phenotype (PMID:19147579)
• The authors provide evidence that TMPRSS2 and TMPRSS4 activate the 1918 HA by cleavage and therefore may promote viral spread in lung tissue. (PMID:19158246)
• Translocation of TMPRSS2-ERG is not associated with outcome and the aggressive clinical features associated with copy number increas in prostate cancer. (PMID:19190343)
• the up-regulation of TMPRSS2 and the down-regulation of KLK11 in advanced and more aggressive tumors may open the feasibility of being used as biomarkers distinguishing the tumor aggressiveness as well as novel prognostic indicators for prostate cancer. (PMID:19242826)
• We found that TMPRSS2-ERG gene fusion is associated with the zonal origin of prostate cancer. (PMID:19396154)
• TMPRSS2:ERG fusion was identified in 83% (15/18), 71% (5/7), 50% (9/18), 33% (3/9), and 29% (5/17) of mucinous, small cell, ductal, glomeruloid, and foamy gland prostate carcinomas, respectively (PMID:19465903)
• Results suggest that androgen ablation inhibits the expression of TMPRSS2:ERG, and that tumors in which pre-surgery androgen ablation fails to suppress expression of the fusion gene have a higher risk of recurrence. (PMID:19494719)
• Rsults show that TMPRSS2-ERG rearrangement is common among North American men who have prostate cancer on biopsy. (PMID:19584163)
• A significantly reduced expression of TMPRSS2 was evident in malignant cells harboring TMPRSS2-ERG fusion, but not in prostate cancer cells without TMPRSS2-ERG fusion, further defining these two genetically distinct types of prostate cancer. (PMID:19597533)
• This study demonstrates that most ERG-overexpressing prostate cancers harbor hormonally regulated TMPRSS2-ERG, SLC45A3-ERG, or NDRG1-ERG fusions (PMID:19649210)
• these findings contribute to the increasing elucidation of the role of TMPRSS2:ERG in the development of prostate cancer. (PMID:19664128)
• SMARCD1/BAF60a is an androgen receptor cofactor that modulates TMPRSS2 expression (PMID:19762545)
• study shows in prostate cancer cells, androgen signaling induces proximity of the TMPRSS2 & ERG genomic loci, located on chromosome 21q22.2; exposure to gamma irradiation, causing DNA double-strand breaks, facilitates formation of TMPRSS2-ERG gene fusion (PMID:19933109)
• TMPRSS2-ERG T1/E4 fusion-positive tumours had differentially regulated mRNAs observed in multiple studies. (PMID:20068566)
• This is the first study to report concurrent TMPRSS2 and SLC45A3 rearrangements in the same tumor focus in prostate cancer (PMID:20118910)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	tmprss2	ENSDARG00000098686
mus_musculus	Tmprss2	ENSMUSG00000000385
rattus_norvegicus	Tmprss2	ENSRNOG00000001976
drosophila_melanogaster	Sb	FBGN0003319
drosophila_melanogaster	CG17242	FBGN0250841

Paralogs (17): PRSS22 (ENSG00000005001), PRSS21 (ENSG00000007038), TMPRSS11E (ENSG00000087128), HPN (ENSG00000105707), TMPRSS13 (ENSG00000137747), ST14 (ENSG00000149418), TMPRSS11D (ENSG00000153802), TMPRSS15 (ENSG00000154646), TMPRSS3 (ENSG00000160183), TMPRSS5 (ENSG00000166682), TMPRSS7 (ENSG00000176040), TMPRSS9 (ENSG00000178297), TMPRSS11B (ENSG00000185873), TMPRSS6 (ENSG00000187045), TMPRSS11A (ENSG00000187054), TMPRSS11F (ENSG00000198092), PRSS41 (ENSG00000215148)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1354381) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 21 distinct phenotype terms.

Mouse phenotype (MP)	Records
decreased susceptibility to Orthomyxoviridae infection	2
decreased susceptibility to Orthomyxoviridae infection induced morbidity/mortality	2
abnormal heart morphology	1
enlarged heart	1
abnormal spleen morphology	1
abnormal thymus morphology	1
enlarged thymus	1
abnormal testis morphology	1
small testis	1
abnormal contextual conditioning behavior	1
lung inflammation	1
abnormal epididymis morphology	1
increased circulating alanine transaminase level	1
abnormal cytokine secretion	1
abnormal auditory brainstem response	1
enlarged epididymis	1
decreased cardiac muscle contractility	1
improved glucose tolerance	1
increased circulating total protein level	1
increased fasting circulating glucose level	1
decreased susceptibility to Coronaviridae infection	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pongo abelii	Q5R5E8	99.3%	Diamond
Pan troglodytes	Q2F9P2	98.7%	Diamond
Pan paniscus	Q2F9P4	98.7%	Diamond
Tachypleus tridentatus	P28175	97.2%	Diamond
Carcinoscorpius rotundicauda	Q26422	97.2%	Diamond
Manduca sexta	P35045	96.1%	Diamond
Macaca mulatta	Q28506	95.7%	Diamond
Oxyuranus microlepidotus	Q58L95	95.1%	Diamond
Pseudonaja textilis	Q1L659	93.6%	Diamond
Tropidechis carinatus	Q4QXT9	93.6%	Diamond
Bos taurus	P06868	92.9%	Diamond
Capra hircus	Q28315	92.7%	Diamond
Rhinella arenarum	Q66TN7	90.6%	Diamond
Bufo japonicus	Q90WD8	90.6%	Diamond
Cryptophis nigrescens	B5G6G5	89.2%	Diamond
Desmodus rotundus	P49150	88.2%	Diamond
Canis lupus familiaris	P04813	87.1%	Diamond
Felis catus	Q28412	86.0%	Diamond
Sus scrofa	P08419	85.9%	Diamond
Demansia vestigiata	A6MFK7	85.8%	Diamond
Acropora millepora	B8VIV4	85.1%	Diamond
Mesocricetus auratus	P15156	84.7%	Diamond
Meriones unguiculatus	P50342	84.7%	Diamond
Equus caballus	Q28380	84.7%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
MX1	protein-coding	4599
MX2	protein-coding	4600
PCSEAT	ncRNA	105372808
FAM3B	protein-coding	54097
PLAC4	ncRNA	191585
BACE2	protein-coding	25825

Protein

Protein identifiers

Transmembrane protease serine 2 — O15393 (reviewed: O15393)

Alternative names: Serine protease 10

All UniProt accessions (11): A0A7I2V3D1, A0A7I2V474, A0A7I2V509, A0A7I2V5F9, A0A7I2V5N2, A0A7I2V650, A0A7I2YQ98, C9J5Y1, C9JB05, C9JKZ3, O15393

UniProt curated annotations — full annotation on UniProt →

Function. Plasma membrane-anchored serine protease that cleaves at arginine residues. Participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia. (Microbial infection) Facilitates human coronaviruses SARS-CoV and SARS-CoV-2 infections via two independent mechanisms, proteolytic cleavage of ACE2 receptor which promotes viral uptake, and cleavage of coronavirus spike glycoproteins which activates the glycoprotein for host cell entry. The cleavage of SARS-COV2 spike glycoprotein occurs between the S2 and S2’ site. Upon SARS-CoV-2 infection, increases syncytia formation by accelerating the fusion process. Proteolytically cleaves and activates the spike glycoproteins of human coronavirus 229E (HCoV-229E) and human coronavirus EMC (HCoV-EMC) and the fusion glycoproteins F0 of Sendai virus (SeV), human metapneumovirus (HMPV), human parainfluenza 1, 2, 3, 4a and 4b viruses (HPIV). Essential for spread and pathogenesis of influenza A virus (strains H1N1, H3N2 and H7N9); involved in proteolytic cleavage and activation of hemagglutinin (HA) protein which is essential for viral infectivity. (Microbial infection) Receptor for human coronavirus HKU1-CoV, acts synergistically with disialoside glycans to facilitate the entry of the virus. After binding to cell-surface disialoside glycans, the viral S protein interacts with the inactive form of TMPRSS2 and inhibits its protease activity.

Subunit / interactions. The catalytically active form interacts with ACE2.

Subcellular location. Cell membrane Secreted.

Tissue specificity. Expressed in several tissues that comprise large populations of epithelial cells with the highest level of transcripts measured in the prostate gland. Expressed in type II pneumocytes in the lung (at protein level). Expressed strongly in small intestine. Also expressed in colon, stomach and salivary gland. Coexpressed with ACE2 within lung type II pneumocytes, ileal absorptive enterocytes, intestinal epithelial cells, cornea, gallbladder and nasal goblet secretory cells (Ref.21).

Post-translational modifications. Proteolytically processed; by an autocatalytic mechanism. Autocleavage induces active conformation.

Induction. By androgenic hormones in vivo.

Similarity. Belongs to the peptidase S1 family.

Isoforms (2)

UniProt ID	Names	Canonical?
O15393-1	1	yes
O15393-2	2

RefSeq proteins (3): NP_001128571, NP_001369649, NP_005647* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001190	SRCR	Domain
IPR001254	Trypsin_dom	Domain
IPR001314	Peptidase_S1A	Family
IPR002172	LDrepeatLR_classA_rpt	Repeat
IPR009003	Peptidase_S1_PA	Homologous_superfamily
IPR018114	TRYPSIN_HIS	Active_site
IPR023415	LDLR_class-A_CS	Conserved_site
IPR033116	TRYPSIN_SER	Active_site
IPR036055	LDL_receptor-like_sf	Homologous_superfamily
IPR036772	SRCR-like_dom_sf	Homologous_superfamily
IPR043504

Pfam: PF00089, PF15494

Enzyme classification (BRENDA)

• EC 3.4.21.122 — transmembrane protease serine 2 (BRENDA: 5 organisms, 49 substrates, 158 inhibitors, 15 Km, 1 kcat entries)
• EC 3.4.21.B60 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

Substrate kinetics (BRENDA)

13 substrates with measured Km, best-characterized 13. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
BOC-LEU-GLY-ARG-7-AMIDO-4-METHYLCOUMARIN	0.075–0.2	2
TERT-BUTYLOXYCARBONYL-L-GLN-L-ALA-L-ARG-7-AMIDO-	0.0095–0.077	2
BOC-PHE-GLY-ARG-7-AMIDO-4-METHYLCOUMARIN	0.094	1
BOC-PHE-SER-ARG-7-AMIDO-4-METHYLCOUMARIN	0.058	1
CH3-O-CO-D-CYCLOHEXYLALANINE-GLY-ARG-4-NITROANIL	0.055	1
CH3-SO2-D-ARG-PRO-ARG-7-AMIDO-4-METHYLCOUMARIN	0.043	1
CH3-SO2-D-CYCLOHEXYLALANINE-GLY-ARG-4-NITROANILI	0.019	1
CH3-SO2-D-CYCLOHEXYLGLYCINE-GLY-ARG-4-NITROANILI	0.026	1
D-CYCLOHEXYLALANINE-GLY-ARG-4-NITROANILIDE	0.059	1
D-HEXAHYDROTYROSINE-GLY-ARG-4-NITROANILIDE	0.065	1
D-PHE-PRO-ARG-7-AMIDO-4-METHYLCOUMARIN	0.087	1
TOS-GLY-PRO-ARG-7-AMIDO-4-METHYLCOUMARIN	0.081	1
TOS-GLY-PRO-LYS-7-AMIDO-4-METHYLCOUMARIN	0.159	1

UniProt features (118 total): strand 29, mutagenesis site 22, helix 15, sequence variant 9, disulfide bond 9, turn 8, binding site 5, sequence conflict 5, active site 3, domain 3, chain 2, glycosylation site 2, topological domain 2, site 1, splice variant 1, transmembrane region 1, region of interest 1

Structure

Experimental structures (PDB)

showing 30 of 34 structures by resolution:

PDB	Title	Method	Resolution (Å)
8V04	High resolution TMPRSS2 structure following acylation by nafamostat	X-RAY DIFFRACTION	1.58
8S0L	Crystal structure of the TMPRSS2 zymogen in complex with the nanobody A07	X-RAY DIFFRACTION	1.8
9JD1	Crystal structure of TMPRSS2 in complex with Fab	X-RAY DIFFRACTION	1.9
7MEQ	Crystal structure of human TMPRSS2 in complex with Nafamostat	X-RAY DIFFRACTION	1.95
9JD0	Crystal structure of TMPRSS2 in complex with nanobody	X-RAY DIFFRACTION	2
9U8G	Crystal structure of TMPRSS2 in complex with nanobody77_10	X-RAY DIFFRACTION	2
9E83	TMPRSS2 crystal structure following acylation by UCSF_157	X-RAY DIFFRACTION	2.07
8V1F	TMPRSS2 complexed with the noncovalent inhibitor 6-amidino-2-napthol	X-RAY DIFFRACTION	2.19
8S0N	Crystal structure of the TMPRSS2 zymogen in complex with the nanobody A07	X-RAY DIFFRACTION	2.3
7Y0E	Crystal structure of TMPRSS2 in complex with Camostat	X-RAY DIFFRACTION	2.39
8HD8	Crystal structure of TMPRSS2 in complex with 212-148	X-RAY DIFFRACTION	2.4
9IZN	Crystal structure of HKU1A RBD bound to TMPRSS2	X-RAY DIFFRACTION	2.4
7XYD	Crystal structure of TMPRSS2 in complex with Nafamostat	X-RAY DIFFRACTION	2.58
7Y0F	Crystal structure of TMPRSS2 in complex with UK-371804	X-RAY DIFFRACTION	2.6
8Y1D	2up-TM conformation of HKU1-B S protein after incubation of the receptor	ELECTRON MICROSCOPY	2.7
8Y1E	3up-TM conformation of HKU1-B S protein after incubation of the receptor	ELECTRON MICROSCOPY	2.7
9JCX	Crystal structure of the HCoV-HKU1 RBD and TMPRSS2	X-RAY DIFFRACTION	2.75
9Z3J	HCoV-NL63 S2’ peptide bound to TMPRSS2 S441A (complexed with the H1H7 Fab and an …	ELECTRON MICROSCOPY	2.8
8VGT	Structure of the HKU1 RBD bound to the human TMPRSS2 receptor	ELECTRON MICROSCOPY	2.9
8JI0	Cryo-EM structure of the TcsH-CROP in complex with TMPRSS2	ELECTRON MICROSCOPY	3
8Y8B	Local structure of HCoV-HKU1C spike in complex with TMPRSS2 and glycan	ELECTRON MICROSCOPY	3.01
8Y88	Structure of HCoV-HKU1C spike in the functionally anchored-2up conformation with 2TMPRSS2	ELECTRON MICROSCOPY	3.03
8Y7X	Structure of HCoV-HKU1A spike in the functionally anchored-3up conformation with 3TMPRSS2	ELECTRON MICROSCOPY	3.09
9K3T	Cryo-EM structure of TMPRSS2 in complex with Fab fragments of 752 mAb and 2228 mAb	ELECTRON MICROSCOPY	3.15
8Y8A	Structure of HCoV-HKU1C spike in the functionally anchored-3up conformation with 3TMPRSS2	ELECTRON MICROSCOPY	3.19
8JHZ	Cryo-EM structure of the TcsH-TMPRSS2 complex	ELECTRON MICROSCOPY	3.2
9OPR	TMPRSS2 S441A in complex with the H1H7 Fab and anti-kappa light chain nanobody	ELECTRON MICROSCOPY	3.2
8YOY	Structure of HKU1A RBD with TMPRSS2	ELECTRON MICROSCOPY	3.21
8Y7Y	Local structure of HCoV-HKU1A spike in complex with TMPRSS2 and glycan	ELECTRON MICROSCOPY	3.24
8Y87	Structure of HCoV-HKU1C spike in the functionally anchored-1up conformation with 1TMPRSS2	ELECTRON MICROSCOPY	3.26

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O15393-F1	79.72	0.51

Antibody-complex structures (SAbDab)

7 antibodies co-crystallized with this protein: 8S0L, 8S0M, 8S0N, 9JD0, 9JD1, 9K3T, 9U8G

Human Protein Atlas

Protein class: Enzymes, Peptidases, Serine-type peptidases, Transporters, Accessory Factors Involved in Transport, Predicted membrane proteins, Predicted secreted proteins, Predicted intracellular proteins, Cancer-related genes, Candidate cancer biomarkers

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): plasma membrane

Antibody reliability (HPA): IH enhanced · IF supported

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (4)

Position	Role
345	charge relay system
441	charge relay system
255–256	cleavage; by autolysis
296	charge relay system

Ligand- & substrate-binding residues (5)

Position	Role
131	Ca(2+)
134	Ca(2+)
136	Ca(2+)
144	Ca(2+)
145	Ca(2+)

Disulfide bonds (9)

Type	Positions
Disulfide bond	113–126, 120–139, 133–148, 172–231, 185–241, 281–297, 410–426, 437–465
Interchain (between non-catalytic and catalytic chains)	244–365

Glycosylation sites (2)

Type	Positions
N-linked (glcnac…) asparagine	213, 249

Mutagenesis-validated functional residues (22)

Position	Phenotype
255	loss of cleavage. no effect on hku1-cov viral entry.
316	no effect on catalytic activity or hku1-cov viral entry.
340	no effect on hku1-cov viral entry.
341	no effect on catalytic activity or hku1-cov viral entry.
409	no effect on catalytic activity. reduces hku1-cov viral entry.
412	no effect on catalytic activity. reduces hku1-cov viral entry.
413	no effect on catalytic activity. reduces hku1-cov viral entry.
414	no effect on catalytic activity. almost abolishes s protein-binding and hku1-cov viral entry.
415	no effect on hku1-cov viral entry.
416	no effect on catalytic activity. almost abolishes hku1-cov viral entry.
417	no effect on catalytic activity. almost abolishes hku1-cov viral entry.
419	no effect on catalytic activity. abolishes hku1-cov viral entry.
430	no effect on catalytic activity. abolishes hku1-cov viral entry.
431	no effect on catalytic activity or hku1-cov viral entry.
433	no effect on catalytic activity or hku1-cov viral entry.
441	loss of activity. no effect on hku1-cov viral entry.
461	no effect on catalytic activity. abolishes hku1-cov s protein-binding and viral entry.
463	no effect on catalytic activity. reduces hku1-cov viral entry.
467	no effect on catalytic activity. reduces hku1-cov viral entry.
468	no effect on hku1-cov viral entry.
469	no effect on catalytic activity. reduces hku1-cov viral entry.
470	no effect on catalytic activity. abolishes hku1-cov s protein-binding and viral entry.

Function

Pathways and Gene Ontology

Reactome pathways

3 curated (TAS) of 11; 11 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

11 pathways:

ID	Pathway	Evidence
R-HSA-9678110	Attachment and Entry ⚕	curated
R-HSA-9694614	Attachment and Entry ⚕	curated
R-HSA-9733458	Induction of Cell-Cell Fusion ⚕	curated
R-HSA-1643685	Disease ⚕	—
R-HSA-9772572	Early SARS-CoV-2 Infection Events ⚕	—
R-HSA-5663205	Infectious disease ⚕	—
R-HSA-9772573	Late SARS-CoV-2 Infection Events ⚕	—
R-HSA-9679506	SARS-CoV Infections ⚕	—
R-HSA-9678108	SARS-CoV-1 Infection ⚕	—
R-HSA-9694516	SARS-CoV-2 Infection ⚕	—
R-HSA-9824446	Viral Infection Pathways ⚕	—

MSigDB gene sets: 172 (showing top): MODULE_172, MODULE_64, RODWELL_AGING_KIDNEY_NO_BLOOD_DN, GOBP_PROTEIN_MATURATION, GOBP_REGULATION_OF_BIOLOGICAL_PROCESS_INVOLVED_IN_SYMBIOTIC_INTERACTION, MODULE_109, MCBRYAN_PUBERTAL_BREAST_3_4WK_UP, CAIRO_HEPATOBLASTOMA_DN, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_UP, GOBP_BIOLOGICAL_PROCESS_INVOLVED_IN_INTERACTION_WITH_HOST, CREIGHTON_ENDOCRINE_THERAPY_RESISTANCE_5, GOBP_VIRAL_LIFE_CYCLE, NELSON_RESPONSE_TO_ANDROGEN_UP, GFI1_01, MULLIGHAN_NPM1_SIGNATURE_3_DN

GO Biological Process (4): proteolysis (GO:0006508), protein autoprocessing (GO:0016540), positive regulation of viral entry into host cell (GO:0046598), entry receptor-mediated virion attachment to host cell (GO:0098670)

GO Molecular Function (5): serine-type endopeptidase activity (GO:0004252), serine-type peptidase activity (GO:0008236), protein binding (GO:0005515), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)

GO Cellular Component (4): extracellular region (GO:0005576), plasma membrane (GO:0005886), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

8 top-level categories:

Category	Pathways
SARS-CoV Infections	2
SARS-CoV-2 Infection	2
SARS-CoV-1 Infection	1
Early SARS-CoV-2 Infection Events	1
Late SARS-CoV-2 Infection Events	1
Disease	1
Viral Infection Pathways	1
Infectious disease	1

GO top-level categories

19 GO namespaces:

Category	Terms
cellular anatomical structure	2
protein metabolic process	1
protein processing	1
regulation of viral entry into host cell	1
symbiont entry into host cell	1
positive regulation by symbiont of entry into host	1
positive regulation of viral life cycle	1
receptor-mediated virion attachment to host cell	1
endopeptidase activity	1
serine-type peptidase activity	1
peptidase activity	1
serine hydrolase activity	1
binding	1
hydrolase activity	1
catalytic activity, acting on a protein	1
catalytic activity	1
membrane	1
cell periphery	1
extracellular vesicle	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 7 of 13 annotations. The rest are phylogenetic / computational / electronic (IEA).

7 experimentally-supported GO terms:

GO term	NS	Evidence
entry receptor-mediated virion attachment to host cell	BP	direct assay
positive regulation of viral entry into host cell	BP	direct assay
protein autoprocessing	BP	mutant phenotype
proteolysis	BP	direct assay
extracellular exosome	CC	high-throughput assay
plasma membrane	CC	direct assay
serine-type endopeptidase activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 2,385 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TMPRSS2	ACE2	Q9BYF1	949
TMPRSS2	ETV1	P50549	915
TMPRSS2	FURIN	P09958	903
TMPRSS2	CTSL	P07711	893
TMPRSS2	ERG	P11308	885
TMPRSS2	AR	P10275	864
TMPRSS2	SLC45A3	Q96JT2	860
TMPRSS2	ACE	P12821	790
TMPRSS2	NRP1	O14786	785
TMPRSS2	CTSB	P07858	767
TMPRSS2	DPP4	P27487	767
TMPRSS2	CTSS	P25774	764
TMPRSS2	BSG	P35613	761
TMPRSS2	REN	P00797	727
TMPRSS2	ADAM17	P78536	720

IntAct

Human interaction partners of TMPRSS2 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

2 partners by confidence:

Partner	Interaction type	MIscore	Records
SERPINA1	cleavage reaction	0.560	2
ACE2	physical association	0.460	3

BioGRID (434 interactions; top human partners by supporting records): ACE2 (Biochemical Activity; 6 records), DDX39B (Proximity Label-MS; 3 records), ABL1 (Affinity Capture-Western; 2 records), ADAM10 (Affinity Capture-MS; 2 records), ADAM15 (Affinity Capture-MS; 2 records), AFG3L2 (Affinity Capture-MS; 2 records), AIF1L (Affinity Capture-MS; 2 records), APP (Affinity Capture-MS; 2 records), ATP1B3 (Affinity Capture-MS; 2 records), CALM2 (Affinity Capture-MS; 2 records), CDH2 (Affinity Capture-MS; 2 records), CLGN (Affinity Capture-MS; 2 records), CLTA (Affinity Capture-MS; 2 records), CPD (Affinity Capture-MS; 2 records), CTSD (Affinity Capture-MS; 2 records)

SIGNOR signaling

showing 6 of 9 signaling interactions:

A	Effect	B	Mechanism
AR	“up-regulates quantity by expression”	TMPRSS2	“transcriptional regulation”
TMPRSS2	“up-regulates activity”	S	cleavage
Camostat	“down-regulates activity”	TMPRSS2	“chemical inhibition”
nafamostat	“down-regulates activity”	TMPRSS2	“chemical inhibition”
“Camostat mesylate”	“down-regulates activity”	TMPRSS2	“chemical inhibition”
TMPRSS2	“up-regulates quantity by expression”	HGF	“transcriptional regulation”

Protein complexes (CORUM) (1)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

1 complexes by size:

Complex	Subunits	Members
ACE2-TMPRSS2 complex	2	ACE2, TMPRSS2

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: activating (oncogene-like) across 1 cancer types — PRAD.

intOGen’s role is a computational inference from cohort mutation patterns and may diverge from the gene’s curated/literature role; read it alongside the evidence above.

Genetic variants

Variant evidence for TMPRSS2: 35 ClinVar records (1 pathogenic / likely pathogenic); 4 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

35 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	11
Likely benign	8
Benign	4

Top pathogenic / likely-pathogenic (1)

Showing all 1 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
1526705	GRCh37/hg19 21q11.2-22.3(chr21:15041209-48097372)x3	Pathogenic	criteria provided, single submitter	1

Per-variant reference — Sugi Variant

Explore TMPRSS2’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 37 predictions of 1,363):

Position(s)	Effect	Δscore	Sites
21:41468394–41468395	donor_loss	1.0000	5
21:41468539–41468540	acceptor_loss	1.0000	6
21:41470744–41470745	acceptor_loss	1.0000	6
21:41470751	acceptor_gain	1.0000
21:41471804–41471805	donor_loss	1.0000	5
21:41473314	donor_gain	1.0000
21:41473323	donor_loss	1.0000	2
21:41476621–41476622	acceptor_loss	1.0000	6
21:41479170–41479171	donor_loss	1.0000	4
21:41488515	acceptor_gain	1.0000

AlphaMissense

925 missense substitutions predicted likely pathogenic (of 3,218 scored), across 220 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M424	9	0.923	0.982
D440	8	0.994	0.999
D345	8	0.993	0.998
D435	8	0.990	0.996
H296	8	0.982	0.994
S441	8	0.974	0.993
S460	8	0.963	0.997
S272	8	0.944	0.997
H279	8	0.941	0.986
D144	8	0.872	0.962
N17	8	0.760	0.911
C437	7	0.998	0.999
W384	7	0.997	0.999
C426	7	0.997	0.999
C465	7	0.996	0.999
C281	7	0.995	0.998
C297	7	0.994	0.997
C410	7	0.994	0.999
C365	7	0.991	0.995
W461	7	0.990	0.999

HPA cancer prognostics

RNA cancer specificity: Cancer enriched (Prostate Adenocarcinoma)

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

2 prognostic cancer types:

Cancer	Prognostic	p-value
Liver Hepatocellular Carcinoma (validation)	favorable	9.91e-05
Lung Adenocarcinoma (TCGA)	favorable	0.00068

Disease associations

OMIM: gene MIM:602060 | disease phenotypes:

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (1 panels, 1 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

1 panels:

Panel	Rating
COVID-19 research	green

GWAS associations

4 associations:

Study	Trait	p-value
GCST90013407_2	Liver enzyme levels (gamma-glutamyl transferase)	3e-16
GCST002337_60	Amyotrophic lateral sclerosis (sporadic)	2e-9
GCST002606_6	Prostate cancer	3e-8
GCST002606_24	Prostate cancer	3e-7

EFO canonical traits (from GWAS)

1 canonical traits:

EFO ID	Trait name
EFO:0004532	serum gamma-glutamyl transferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1795140 (SINGLE PROTEIN), CHEMBL6195526 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 79,134 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

9 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL169901	DEBRISOQUIN	4	1,072
CHEMBL55	PENTAMIDINE	4	27,197
CHEMBL506247	TANNIC ACID	4	27,154
CHEMBL590799	CAMOSTAT	3	6,825
CHEMBL87563	GABEXATE	3	2,044
CHEMBL273264	NAFAMOSTAT	3	7,150
CHEMBL46618	OTAMIXABAN	3	548
CHEMBL23013	PROPAMIDINE	3	5,144
CHEMBL35241	DIMINAZENE	2	2,000

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

1 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs383510		Other	Genotype CC is associated with increased likelihood of COVID-19 as compared to genotypes CT + TT.	PMID:33968142

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — S1: Chymotrypsin

Most potent curated ligand interactions (8 total), top 8:

Ligand	Action	Affinity	Parameter
N-0920	Inhibition	9.46	pIC50
MM3122	Inhibition	9.37	pIC50
I-432	Inhibition	9.05	pKi
N-0385	Inhibition	8.72	pIC50
compound 5 [PMID: 21741839]	Inhibition	7.7	pKi
nafamostat	Inhibition	7.0	pIC50
otamixaban	Inhibition	6.21	pIC50
camostat	Inhibition	6.0	pIC50

Binding affinities (BindingDB)

54 measured of 71 human assays (82 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL6163291	KI	0.16 nM
CHEMBL6174967	IC50	0.35 nM
Otamixaban	KI	0.4 nM
CHEMBL6150218	IC50	0.62 nM
CHEMBL6164098	IC50	0.66 nM
CHEMBL6176630	IC50	0.66 nM
CHEMBL6167030	IC50	0.74 nM
CHEMBL6172466	IC50	0.87 nM
CHEMBL3219079	KI	0.9 nM
CHEMBL3219087	KI	1 nM
CHEMBL6159875	IC50	1 nM
CHEMBL6165833	IC50	1.3 nM
CHEMBL6142154	IC50	1.4 nM
CHEMBL6132920	IC50	1.4 nM
CHEMBL6160234	IC50	1.4 nM
CHEMBL1809250	KI	2.1 nM
Benzylsulfonyl-D-argininyl-proline-(4-amidinobenzyl)amide Bis-(trifluoroacetate)	KI	2.4 nM
CHEMBL3219102	KI	3 nM
CHEMBL3219101	KI	3 nM
CHEMBL3219100	KI	3 nM
CHEMBL3219103	KI	3 nM
CHEMBL6164215	IC50	3.2 nM
CHEMBL6163067	KI	9.2 nM
(4S,4’S)-6-chloro-4,-[(ethylamino)methyl]-1,-(4-isoquinolyl)-2-[(3-methylisoxazol-5-yl)methyl]spiro[3H-isoquinoUne-4,3’-pyrrolidine]-1,2,-dione	EC50	15 nM	WO-2025125695: CHEMICAL COMPOUNDSID50000167790940 P. DOC 2025-05-07 FILING NO.:19
(4S,4’S)-6-chloro-4,-[(ethylamino)methyl]-1,-(4-isoquinolyl)-2-[(tetrahydropyran-4-ylmethyl)]spiro[3H-isoquinoUne-4,3’-pyrrolidine]-1,2,-dione	EC50	18 nM	WO-2025125695: CHEMICAL COMPOUNDSID50000167790940 P. DOC 2025-05-07 FILING NO.:19
(4S,4’S)-6-chloro-4,-[(ethylamino)methyl]-1,-(4-isoquinolyl)-2-[(6-methylpyrimidin-4-yl)methyl]spiro[3H-isoquinoUne-4,3’-pyrrolidine]-1,2,-dione	EC50	31 nM	WO-2025125695: CHEMICAL COMPOUNDSID50000167790940 P. DOC 2025-05-07 FILING NO.:19
(4S,4’S)-6-chloro-4’-[(isopropylamino)methyl]-1’-(4-isoquinolyl)-2-[(1-methyltriazol-4-yl)methyl]spiro[3H-isoquinoUne-4,3’-pyrrolidine]-1,2,-dione	EC50	34 nM	WO-2025125695: CHEMICAL COMPOUNDSID50000167790940 P. DOC 2025-05-07 FILING NO.:19
CHEMBL1809251	KI	37 nM
CHEMBL1185793	IC50	70 nM
(4S,4’S)-6-chloro-4,-[(ethylamino)methyl]-1,-(4-isoquinolyl)-2-[(6-methylpyrimidin-4-yl)methyl]spiro[3H-isoquinoUne-4,3’-pyrrolidine]-1,2,-dione	EC50	76 nM	WO-2025125695: CHEMICAL COMPOUNDSID50000167790940 P. DOC 2025-05-07 FILING NO.:19
CHEMBL6172535	KI	102 nM
CHEMBL5557551	IC50	250 nM
Bromhexine	IC50	750 nM
0591-5329	IC50	930 nM
(7-Hydroxy-2-oxo-2H-chromen-4-yl)-acetic acid methyl ester	IC50	1370 nM
CHEMBL4081543	KI	2320 nM
8008-1235	IC50	2640 nM
4401-0077	IC50	2680 nM
CHEMBL5285196	IC50	3400 nM
CHEMBL5558228	IC50	3980 nM
CHEMBL5270157	IC50	4000 nM
CHEMBL5266850	IC50	4000 nM
4-(6-Guanidino-hexanoyloxy)-benzoic acid ethyl ester	IC50	4610 nM
CHEMBL5271456	IC50	9000 nM
CHEMBL5287275	IC50	12000 nM
CHEMBL5568169	IC50	13000 nM
CHEMBL5559738	IC50	14600 nM
CHEMBL5560415	IC50	19900 nM
CHEMBL5275059	IC50	20000 nM
CHEMBL5270536	IC50	20000 nM

ChEMBL bioactivities

75 potent at pChembl≥5 of 82 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.52	Ki	0.03	nM	CHEMBL6174967
10.02	Ki	0.095	nM	CHEMBL6144144
9.96	Ki	0.11	nM	CHEMBL6172535
9.76	Ki	0.172	nM	CHEMBL5532456
9.62	Ki	0.24	nM	CHEMBL6163067
9.46	IC50	0.35	nM	CHEMBL6174967
9.30	IC50	0.5	nM	NAFAMOSTAT
9.28	Ki	0.53	nM	CHEMBL6163291
9.23	IC50	0.59	nM	CHEMBL6172535
9.23	IC50	0.59	nM	CHEMBL6174967
9.21	IC50	0.62	nM	CHEMBL6150218
9.18	IC50	0.66	nM	CHEMBL6164098
9.18	IC50	0.66	nM	CHEMBL6176630
9.17	IC50	0.67	nM	CHEMBL5532456
9.13	IC50	0.74	nM	CHEMBL6167030
9.06	IC50	0.87	nM	CHEMBL6172466
9.06	IC50	0.87	nM	CHEMBL6163067
9.05	Ki	0.9	nM	CHEMBL3219079
9.05	IC50	0.89	nM	CHEMBL6144144
9.01	IC50	0.98	nM	CHEMBL5560415
9.00	Ki	1	nM	CHEMBL3219087
9.00	IC50	1	nM	NAFAMOSTAT
9.00	IC50	1	nM	CHEMBL6159875
8.92	IC50	1.2	nM	CHEMBL5558547
8.92	IC50	1.2	nM	CHEMBL5557551
8.89	IC50	1.3	nM	CHEMBL6165833
8.85	IC50	1.4	nM	CHEMBL5982921
8.85	IC50	1.4	nM	CHEMBL6142154
8.85	IC50	1.4	nM	CHEMBL6132920
8.85	IC50	1.4	nM	CHEMBL6160234
8.77	IC50	1.7	nM	CHEMBL5620212
8.72	IC50	1.9	nM	CHEMBL5532456
8.62	IC50	2.4	nM	CHEMBL6163291
8.60	IC50	2.5	nM	CHEMBL5555448
8.52	Ki	3	nM	CHEMBL3219102
8.52	Ki	3	nM	CHEMBL3219101
8.52	Ki	3	nM	CHEMBL3219100
8.52	Ki	3	nM	CHEMBL3219103
8.52	IC50	3	nM	CHEMBL4081543
8.49	IC50	3.2	nM	CHEMBL6164215
8.43	IC50	3.7	nM	CHEMBL5559738
8.41	IC50	3.9	nM	CAMOSTAT
8.38	IC50	4.2	nM	CHEMBL5559988
8.38	IC50	4.2	nM	CHEMBL5619680
8.01	IC50	9.8	nM	CHEMBL5560759
7.96	IC50	11	nM	CHEMBL5568169
7.92	Ki	12	nM	CHEMBL6172535
7.92	Ki	12	nM	CHEMBL6144144
7.92	Ki	12	nM	CHEMBL6163067
7.92	Ki	12	nM	CHEMBL6174967

PubChem BioAssay actives

85 with measured affinity, of 133 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
benzyl N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamate	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	<0.0001	uM
ethyl N-[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamate	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(3-methoxypropanoylamino)pentanediamide	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	0.0001	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(methanesulfonamido)pentanediamide	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	0.0002	uM
(2S)-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(methanesulfonamido)pentanediamide	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	0.0002	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]pentanediamide	2240384: Inhibition of recombinant das TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells assessed as inhibition constant using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ki	0.0005	uM
(6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate	2067026: Inhibition of human TMPRSS2	ic50	0.0005	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]-N’,N’-dimethylpentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0006	uM
N-[(2S)-1-[[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0007	uM
(2S)-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0007	uM
N-[(2S)-1-[[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-5-(diaminomethylideneamino)pentanamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0007	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]butanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0009	uM
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]-3-oxopropyl]benzenecarboximidamide	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0009	uM
(4Z,7S,10R,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(1H-indol-3-ylmethyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),4,15,18-tetraene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0010	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-5,10-dioxo-1,6-diazecane-2-carboxamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0010	uM
3-[(2S)-3-[4-(2-aminoethyl)piperidin-1-yl]-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]-3-oxopropyl]benzenecarboximidamide	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0010	uM
(8S,11S,14S)-14-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-11-(2-methylpropyl)-10,13-dioxo-2-oxa-9,12-diazatricyclo[14.2.2.23,6]docosa-1(18),3(22),4,6(21),16,19-hexaene-8-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0012	uM
(4E,7S,10S,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(2-methylpropyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),4,15,18-tetraene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0012	uM
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0013	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0014	uM
(2R)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0014	uM
benzyl N-[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamate	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0014	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-(3-hydroxypropanoylamino)pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0014	uM
N-[7-[(2R,3R,4S,5R)-2-cyano-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrrolo[2,1-f][1,2,4]triazin-4-yl]-4-(diaminomethylideneamino)benzamide	2128376: Inhibition of human TMPRSS2 using fluorogenic substrate preincubated with enzyme in dark for 45 mins followed by substrate addition and measured after 10 mins by fluorogenic assay	ic50	0.0017	uM
(4Z,11S,14S,17S)-17-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-14-(2-methylpropyl)-8,13,16-trioxo-2-oxa-7,12,15-triazabicyclo[17.2.2]tricosa-1(21),4,19,22-tetraene-11-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0025	uM
(2S)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-methyl-2-[[(2S)-2-(3-phenylpropanoylamino)-3-(1,3-thiazol-4-yl)propanoyl]amino]butanamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0030	uM
1-[2-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]ethyl]-3-methylurea	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0030	uM
1-[2-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]ethyl]-3-methylurea	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0030	uM
1-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dimethoxyphenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]-3-cyclohexylurea	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0030	uM
1-[1-[(2S)-3-(3-carbamimidoylphenyl)-2-[[3-(2,4-dichlorophenyl)phenyl]sulfonylamino]propanoyl]piperidin-4-yl]-3-cyclohexylurea	1916558: Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method	ki	0.0030	uM
(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pentanediamide	1806088: TMPRSS2 pericellular activity screening assay from Article 10.1038/s41586-022-04661-w: “A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.”	ic50	0.0031	uM
(2S)-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]-2-[5-(diaminomethylideneamino)pentanoylamino]pentanediamide	2240380: Inhibition of recombinant TMPRSS2 (unknown origin) extracted from baculovirus infected in Sf9 cells using Boc-QAR-AMC as substrate measured after 1 hr by fluorescence based analysis	ic50	0.0032	uM
(7S,10R,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(1H-indol-3-ylmethyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-triene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0037	uM
(2S)-2-acetamido-N-[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pentanediamide	1806088: TMPRSS2 pericellular activity screening assay from Article 10.1038/s41586-022-04661-w: “A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.”	ic50	0.0039	uM
[4-[2-[2-(dimethylamino)-2-oxoethoxy]-2-oxoethyl]phenyl] 4-(diaminomethylideneamino)benzoate	2067026: Inhibition of human TMPRSS2	ic50	0.0039	uM
(2-oxo-4-propan-2-ylchromen-6-yl) 4-(diaminomethylideneamino)benzoate	2128376: Inhibition of human TMPRSS2 using fluorogenic substrate preincubated with enzyme in dark for 45 mins followed by substrate addition and measured after 10 mins by fluorogenic assay	ic50	0.0042	uM
(6R,9S,12S)-12-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-9-(2-methylpropyl)-8,11-dioxo-1,7,10,15,16-pentazabicyclo[12.2.1]heptadeca-14(17),15-diene-6-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0042	uM
(4S)-4-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid	1806088: TMPRSS2 pericellular activity screening assay from Article 10.1038/s41586-022-04661-w: “A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.”	ic50	0.0052	uM
(7S,10S,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(2-methylpropyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-triene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0098	uM
(9S,12S,15S)-15-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-12-(2-methylpropyl)-11,14-dioxo-2-oxa-10,13-diazatricyclo[15.2.2.13,7]docosa-1(19),3,5,7(22),17,20-hexaene-9-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0110	uM
(4E,7S,10S,13S)-7-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(2-methylpropyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.2.2]nonadeca-1(17),4,15,18-tetraene-13-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0140	uM
(9S,12S,15S)-9-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-12-(2-methylpropyl)-10,13-dioxo-2-oxa-11,14-diazatricyclo[15.2.2.13,7]docosa-1(19),3,5,7(22),17,20-hexaene-15-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0150	uM
(6S,9S,12R)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-9-(2-methylpropyl)-7,10-dioxo-1,8,11,15,16-pentazabicyclo[12.2.1]heptadeca-14(17),15-diene-12-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0150	uM
(7S,10S,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-(1H-indol-3-ylmethyl)-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-triene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0160	uM
(7S,10S,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-10-benzyl-9,12-dioxo-2-oxa-8,11-diazabicyclo[13.2.2]nonadeca-1(17),15,18-triene-7-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0160	uM
(2S)-1-[(2R)-2-(benzylsulfonylamino)-5-(diaminomethylideneamino)pentanoyl]-N-[(4-carbamimidoylphenyl)methyl]pyrrolidine-2-carboxamide	610101: Inhibition of recombinant catalytic domain of TMPRSS2 expressed in Escherichia coli using Dcyclohexylalanine- Pro-Arg-AMC as substrate by fluorescence plate reader analysis	ki	0.0200	uM
(4Z,10S,13S,16S)-16-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-13-(2-methylpropyl)-8,12,15-trioxo-2-oxa-7,11,14-triazabicyclo[16.2.2]docosa-1(20),4,18,21-tetraene-10-carboxamide	2081779: Inhibition of N-terminal 6His-tagged human recombinant TMPRSS2 (106 to 492 residues) using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition and measured by fluorescence based analysis	ic50	0.0220	uM
4-[[[(5R)-5-(benzylsulfonylamino)-8-(diaminomethylideneamino)-4-oxooctan-3-yl]amino]methyl]benzenecarboximidamide	610101: Inhibition of recombinant catalytic domain of TMPRSS2 expressed in Escherichia coli using Dcyclohexylalanine- Pro-Arg-AMC as substrate by fluorescence plate reader analysis	ki	0.0530	uM
4-[[[(4S,6R)-6-(benzylsulfonylamino)-9-(diaminomethylideneamino)-5-oxononan-4-yl]amino]methyl]benzenecarboximidamide	610101: Inhibition of recombinant catalytic domain of TMPRSS2 expressed in Escherichia coli using Dcyclohexylalanine- Pro-Arg-AMC as substrate by fluorescence plate reader analysis	ki	0.0680	uM
2-[4-[4-(diaminomethylideneamino)benzoyl]oxyphenyl]acetic acid	2067026: Inhibition of human TMPRSS2	ic50	0.0700	uM

CTD chemical–gene interactions

128 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Dihydrotestosterone	decreases reaction, increases expression, affects binding, increases reaction, decreases expression	7
Estradiol	affects cotreatment, increases expression, decreases expression, increases reaction	6
Valproic Acid	affects cotreatment, increases expression, affects expression	6
Ethinyl Estradiol	affects expression, decreases expression, increases expression	4
bicalutamide	decreases reaction, increases expression, affects cotreatment, decreases expression	3
Benzo(a)pyrene	decreases expression, increases methylation	3
Testosterone	affects cotreatment, decreases expression, decreases reaction, increases expression	3
Metribolone	decreases reaction, increases expression, decreases expression	3
bisphenol A	affects expression, affects cotreatment, increases methylation	2
sodium arsenite	affects expression, decreases expression	2
entinostat	affects cotreatment, increases expression	2
Acetaminophen	decreases expression	2
Calcitriol	increases expression, affects cotreatment	2
Curcumin	decreases reaction, increases reaction, decreases expression, affects binding	2
Doxorubicin	increases expression, decreases expression	2
Flutamide	decreases reaction, increases expression	2
Nickel	decreases expression	2
Phenobarbital	affects expression, increases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
Tretinoin	affects expression, increases expression	2
Aflatoxin B1	affects expression, decreases expression	2
Genistein	decreases expression	2
dicrotophos	decreases expression	1
androstane-3,17-dione	increases expression	1
eriodictyol	increases cleavage	1
methylselenic acid	affects expression	1
tetramethrin	increases expression	1
2-methyl-4-isothiazolin-3-one	increases expression	1
phentin acetate	affects expression	1

ChEMBL screening assays

28 unique, capped per target: 28 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1810435	Binding	Inhibition of recombinant catalytic domain of TMPRSS2 expressed in Escherichia coli using Dcyclohexylalanine- Pro-Arg-AMC as substrate by fluorescence plate reader analysis	Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT. — *Bioorg Med Chem Lett*

Cellosaurus cell lines

37 cell lines: 28 cancer cell line, 6 spontaneously immortalized cell line, 3 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_0290	HCC1937	Cancer cell line	Female
CVCL_1108	CAL-33	Cancer cell line	Male
CVCL_1576	NCI-H660	Cancer cell line	Male
CVCL_1982	CL-40	Cancer cell line	Female
CVCL_2067	HDQ-P1	Cancer cell line	Female
CVCL_2235	VCaP	Cancer cell line	Male
CVCL_A0BX	VCaP-CR	Cancer cell line	Male
CVCL_A1BP	VCaP AR-V7/pHag	Cancer cell line	Male
CVCL_A5KB	A549-hACE2-TMPRSS2	Cancer cell line	Male
CVCL_A5TF	sciCHO:hACE2:hTMPRSS2	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

showing 60 of 300 trials:

NCT	Phase	Status	Title
NCT00029224	Phase 4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	Phase 4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	Phase 4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	Phase 4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	Phase 4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	Phase 4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	Phase 4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	Phase 4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	Phase 4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	Phase 4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	Phase 4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	Phase 4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	Phase 4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	Phase 4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	Phase 4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	Phase 4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	Phase 4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	Phase 4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	Phase 4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	Phase 4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	Phase 4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	Phase 4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	Phase 4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	Phase 4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	Phase 4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	Phase 4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	Phase 4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	Phase 4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	Phase 4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	Phase 4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	Phase 4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	Phase 4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	Phase 4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	Phase 4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	Phase 4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	Phase 4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	Phase 4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	Phase 4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	Phase 4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	Phase 4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer
NCT01673984	Phase 4	TERMINATED	GP Extended Action Triptorelin
NCT01753297	Phase 4	COMPLETED	A Study of Immediate 9 Months Adjuvant Hormone Therapy With Triptorelin 11.25 mg Versus Active Surveillance After Radical Prostatectomy in High Risk Prostate Cancer Patients.
NCT01794793	Phase 4	COMPLETED	Study to Allow Access to Pasireotide for Patients Benefiting From Pasireotide Treatment in Novartis-sponsored Studies
NCT01950871	Phase 4	TERMINATED	Prostate Guided Biopsy Study Evaluating the Diagnostic Performance of Prostate HistoScanning
NCT01995513	Phase 4	COMPLETED	Safety Study of Continued Enzalutamide Treatment In Prostate Cancer Patients
NCT02102646	Phase 4	COMPLETED	MRI Substudy; Metabolic Changes Due to Iatrogenic Hypogonadism
NCT02116582	Phase 4	COMPLETED	A Study to Evaluate Enzalutamide After Abiraterone in Metastatic Castration-Resistant Prostate Cancer
NCT02149628	Phase 4	COMPLETED	The Effect of Propofol Based Total Intravenous Anesthesia on Oxidative Stress and Nitric Oxide
NCT02405858	Phase 4	COMPLETED	A Study of Abiraterone Acetate in Metastatic Castration-Resistant Prostate Cancer Participants Who Responded Poorly to the First-line Combined Androgen Blockade Therapy
NCT02441517	Phase 4	TERMINATED	A Study of Enzalutamide Re-treatment in Metastatic Castration-resistant Prostate Cancer After Docetaxel and/or Cabazitaxel Treatment
NCT02441894	Phase 4	COMPLETED	Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
NCT02475057	Phase 4	COMPLETED	Endothelial Function in Prostate Cancer Patients on Degarelix vs. Luteinizing Hormone-Releasing Hormone Agonists
NCT02511665	Phase 4	UNKNOWN	Metformin And Longevity
NCT02651948	Phase 4	COMPLETED	Transperineal, MRI-guided, Prostate Biopsy
NCT02721433	Phase 4	COMPLETED	4-weekly Versus 12-weekly Administration of Bone-targeted Agents in Patients With Bone Metastases
NCT02726009	Phase 4	COMPLETED	A Trial to Evaluate Safety of Firmagon® (Degarelix) in Indian Patients Diagnosed With Advanced Hormone-dependent Prostate Cancer
NCT02749825	Phase 4	TERMINATED	Comparison of Trelstar Versus Lupron or Zoladex in Advanced Prostate Cancer
NCT02757365	Phase 4	UNKNOWN	Efficiency Study of Aspirin to Prevent the Occurrence of Prostate Cancer
NCT02773251	Phase 4	COMPLETED	The Effect of Guardix-solution for the Prevention of Postoperative Intestinal Adhesion and Intestinal Obstruction After Laparoscopic Pelvic Cavity Surgery
NCT02812186	Phase 4	COMPLETED	Deep Versus Moderate Neuromuscular Blockade During Laparoscopic Surgery

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for TMPRSS2 across ~30M SureChEMBL compounds — explore on Sugi Predict.