SENP7

gene
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Summary

SENP7 (SUMO specific peptidase 7, HGNC:30402) is a protein-coding gene on chromosome 3q12.3, encoding Sentrin-specific protease 7 (Q9BQF6). Protease that acts as a positive regulator of the cGAS-STING pathway by catalyzing desumoylation of CGAS.

The reversible posttranslational modification of proteins by the addition of small ubiquitin-like SUMO proteins (see SUMO1; MIM 601912) is required for many cellular processes. SUMO-specific proteases, such as SENP7, process SUMO precursors to generate a C-terminal diglycine motif required for the conjugation reaction. They also display isopeptidase activity for deconjugation of SUMO-conjugated substrates (Lima and Reverter, 2008 [PubMed 18799455]).

Source: NCBI Gene 57337 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): arthrogryposis multiplex congenita (Strong, GenCC)
  • GWAS associations: 16
  • Clinical variants (ClinVar): 137 total — 1 pathogenic, 2 likely-pathogenic
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_020654

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:30402
Approved symbolSENP7
NameSUMO specific peptidase 7
Location3q12.3
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000138468
Ensembl biotypeprotein_coding
OMIM612846
Entrez57337

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 9 protein_coding, 1 retained_intron

ENST00000314261, ENST00000348610, ENST00000366089, ENST00000394085, ENST00000394091, ENST00000394094, ENST00000394095, ENST00000460107, ENST00000958688, ENST00000958689

RefSeq mRNA: 5 — MANE Select: NM_020654 NM_001077203, NM_001282801, NM_001282802, NM_001282803, NM_020654

CCDS: CCDS2941, CCDS43121, CCDS63704, CCDS63705, CCDS63706

Canonical transcript exons

ENST00000394095 — 24 exons

ExonStartEnd
ENSE00000934102101327666101327816
ENSE00000934103101328478101328546
ENSE00000934104101328646101328689
ENSE00000934105101330334101330386
ENSE00000934106101331985101332109
ENSE00000967262101398861101399055
ENSE00000967263101372008101372126
ENSE00000967264101367830101368011
ENSE00000967265101366430101366769
ENSE00000967266101364834101364991
ENSE00000967267101361715101361861
ENSE00000967269101343686101343954
ENSE00000967270101341646101341779
ENSE00000967271101340095101340211
ENSE00000967272101337509101337631
ENSE00000967273101332770101332862
ENSE00001014442101351618101351651
ENSE00001209748101458955101459052
ENSE00001252388101347872101348051
ENSE00001386624101417593101417790
ENSE00001866860101324205101326080
ENSE00003493796101513091101513212
ENSE00003560172101501070101501119
ENSE00003668679101493873101493968

Expression profiles

Bgee: expression breadth ubiquitous, 261 present calls, max score 95.15.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 12.4218 / max 229.6578, expressed in 1693 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
4354510.71621656
435441.3899679
435430.3158165

Top tissues by expression

285 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
calcaneal tendonUBERON:000370195.15gold quality
adrenal tissueUBERON:001830391.87gold quality
left ovaryUBERON:000211991.81gold quality
right ovaryUBERON:000211891.60gold quality
ganglionic eminenceUBERON:000402391.22gold quality
ventricular zoneUBERON:000305391.00gold quality
tibiaUBERON:000097990.82gold quality
body of uterusUBERON:000985390.55gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047390.46gold quality
right uterine tubeUBERON:000130290.43gold quality
mucosa of stomachUBERON:000119990.38gold quality
tibial nerveUBERON:000132390.27gold quality
endothelial cellCL:000011590.25gold quality
left uterine tubeUBERON:000130390.02gold quality
cortical plateUBERON:000534389.76gold quality
ovaryUBERON:000099289.75gold quality
endometriumUBERON:000129589.68gold quality
body of pancreasUBERON:000115089.48gold quality
mucosa of paranasal sinusUBERON:000503089.20gold quality
endocervixUBERON:000045888.60gold quality
corpus callosumUBERON:000233688.50gold quality
germinal epithelium of ovaryUBERON:000130488.28gold quality
sural nerveUBERON:001548888.08gold quality
descending thoracic aortaUBERON:000234587.91gold quality
lymph nodeUBERON:000002987.89gold quality
right hemisphere of cerebellumUBERON:001489087.59gold quality
monocyteCL:000057687.57gold quality
tendonUBERON:000004387.30gold quality
ectocervixUBERON:001224987.25gold quality
subcutaneous adipose tissueUBERON:000219087.14gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes5.15

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

83 targeting SENP7, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-3646100.0073.565283
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-MIR-5692A100.0074.406850
HSA-MIR-8485100.0077.574731
HSA-MIR-1277-5P100.0073.955056
HSA-MIR-340-5P100.0072.504437
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-428299.9975.366408
HSA-MIR-477599.9875.006394
HSA-MIR-50799.9770.111915
HSA-MIR-3065-5P99.9771.563281
HSA-MIR-590-3P99.9674.346478
HSA-MIR-55799.9670.011640
HSA-MIR-365899.9673.874379
HSA-MIR-548AJ-3P99.9673.385345
HSA-MIR-548X-3P99.9673.385345
HSA-MIR-4666A-3P99.9671.713434
HSA-MIR-448799.9664.581252
HSA-MIR-545-3P99.9570.742783
HSA-LET-7C-3P99.9573.422862
HSA-MIR-651-3P99.9473.485177
HSA-MIR-548J-3P99.9472.614881
HSA-MIR-314399.9371.963104
HSA-MIR-548AE-3P99.9372.664867
HSA-MIR-548AH-3P99.9372.544872
HSA-MIR-548AM-3P99.9372.544872
HSA-MIR-548AQ-3P99.9372.664867
HSA-MIR-338-5P99.9272.342951

Literature-anchored findings (GeneRIF, showing 9)

  • SENP6 and SENP7 exhibit lower rates for processing pre-SUMO1, pre-SUMO2, or pre-SUMO3 in comparison with SENP2 (PMID:18799455)
  • Loop 1 insertion in SENP6 and SENP7 as a platform to discriminate between SUMO1 and SUMO2/3 isoforms in this subclass of the SUMO protease family. (PMID:21878624)
  • differential splicing of the SENP7 regulates either tumor suppression or progression (PMID:23045645)
  • deSUMOylation by SENP7 is required to promote a permissive chromatin environment for DNA repair. (PMID:24018422)
  • c-Myc is targeted to the proteasome for degradation in a SUMOylation-dependent manner, regulated by PIAS1, SENP7 and RNF4 (PMID:25895136)
  • non-tumorigenic MCF10-2A cells with reduced SENP7S exhibit greater cell proliferation and anchorage-dependent growth. SENP7S depletion directly potentiates tumorigenic properties of MCF10-2A cells with induction of anchorage-independent growth and self-renewal in 3D-spheroid conditions. Collectively, the results identify SENP7S as a novel mediator of beta-catenin signaling and normal mammary epithelial cell physiology. (PMID:28429743)
  • SPOP inhibits hepatocellular carcinoma (HCC) cell metastasis via ubiquitin-dependent SENP7 proteolysis and may thus serve as a new opinion for the prevention of HCC metastasis. (PMID:29777712)
  • DeSUMOylase SENP7-Mediated Epithelial Signaling Triggers Intestinal Inflammation via Expansion of Gamma-Delta T Cells. (PMID:31825833)
  • SENP7 senses oxidative stress to sustain metabolic fitness and antitumor functions of CD8+ T cells. (PMID:35143421)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_reriosenp7bENSDARG00000061138
danio_reriosi:dkey-100n23.3ENSDARG00000062148
mus_musculusSenp7ENSMUSG00000052917
drosophila_melanogasterpiraFBGN0030420
caenorhabditis_elegansWBGENE00006739

Paralogs (1): SENP6 (ENSG00000112701)

Protein

Protein identifiers

Sentrin-specific protease 7Q9BQF6 (reviewed: Q9BQF6)

Alternative names: SUMO-1-specific protease 2, Sentrin/SUMO-specific protease SENP7

All UniProt accessions (3): Q9BQF6, H7C1X8, J3QT09

UniProt curated annotations — full annotation on UniProt →

Function. Protease that acts as a positive regulator of the cGAS-STING pathway by catalyzing desumoylation of CGAS. Desumoylation of CGAS promotes DNA-binding activity of CGAS, subsequent oligomerization and activation. Deconjugates SUMO2 and SUMO3 from targeted proteins, but not SUMO1. Catalyzes the deconjugation of poly-SUMO2 and poly-SUMO3 chains. Has very low efficiency in processing full-length SUMO proteins to their mature forms.

Subcellular location. Cytoplasm.

Similarity. Belongs to the peptidase C48 family.

Isoforms (5)

UniProt IDNamesCanonical?
Q9BQF6-11yes
Q9BQF6-22
Q9BQF6-33
Q9BQF6-44
Q9BQF6-55

RefSeq proteins (5): NP_001070671, NP_001269730, NP_001269731, NP_001269732, NP_065705* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR003653Peptidase_C48_CDomain
IPR038765Papain-like_cys_pep_sfHomologous_superfamily
IPR051947Sentrin-specific_proteaseFamily

Pfam: PF02902

Enzyme classification (BRENDA):

  • EC 3.4.22.B75 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

UniProt features (62 total): helix 12, strand 9, modified residue 8, compositionally biased region 7, sequence conflict 7, region of interest 5, splice variant 5, active site 3, sequence variant 2, mutagenesis site 2, chain 1, turn 1

Structure

Experimental structures (PDB)

2 structures.

PDBMethodResolution (Å)
7R2EX-RAY DIFFRACTION1.74
3EAYX-RAY DIFFRACTION2.4

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9BQF6-F157.050.25

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 (3): 860; 939; 992 (nucleophile)

Post-translational modifications (8): 11, 12, 13, 25, 373, 433, 443, 444

Mutagenesis-validated functional residues (2):

PositionPhenotype
775slightly increased deconjugation activity.
779reduces deconjugation activity.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 143 (showing top): GSE45365_NK_CELL_VS_CD11B_DC_UP, TGCGCANK_UNKNOWN, ATGCAGT_MIR217, GOBP_PROTEIN_MODIFICATION_BY_SMALL_PROTEIN_REMOVAL, GOBP_PEPTIDYL_LYSINE_MODIFICATION, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM, GOMF_CYSTEINE_TYPE_PEPTIDASE_ACTIVITY, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GOBP_DEFENSE_RESPONSE_TO_VIRUS, NOUZOVA_TRETINOIN_AND_H4_ACETYLATION, GOBP_RESPONSE_TO_VIRUS, GOCC_POSTSYNAPSE, GOCC_SYNAPSE, LEE_RECENT_THYMIC_EMIGRANT, GOBP_PROTEOLYSIS

GO Biological Process (5): proteolysis (GO:0006508), protein desumoylation (GO:0016926), antiviral innate immune response (GO:0140374), immune system process (GO:0002376), innate immune response (GO:0045087)

GO Molecular Function (5): SUMO-specific endopeptidase activity (GO:0070139), protein binding (GO:0005515), peptidase activity (GO:0008233), cysteine-type peptidase activity (GO:0008234), hydrolase activity (GO:0016787)

GO Cellular Component (4): nucleus (GO:0005634), cytoplasm (GO:0005737), presynaptic cytosol (GO:0099523), postsynaptic cytosol (GO:0099524)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cytosol2
protein metabolic process1
peptidyl-lysine modification1
protein modification by small protein removal1
innate immune response1
defense response to virus1
biological_process1
immune response1
defense response to symbiont1
ubiquitin-like protein-specific endopeptidase activity1
binding1
hydrolase activity1
catalytic activity, acting on a protein1
peptidase activity1
catalytic activity1
intracellular membrane-bounded organelle1
intracellular anatomical structure1
cellular anatomical structure1
presynapse1
postsynapse1

Protein interactions and networks

STRING

1566 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
SENP7SUMO2P55855902
SENP7RANGAP1P46060900
SENP7SUMO1P55856890
SENP7UBE2IP50550678
SENP7SAE1Q9UBE0673
SENP7RAP2AP10114657
SENP7SENP8Q96LD8651
SENP7DESI1Q6ICB0645
SENP7CBX5P45973631
SENP7RAP1AP10113617
SENP7UBA2Q9UBT2605
SENP7USPL1Q5W0Q7604
SENP7RNF4P78317579
SENP7DESI2Q9BSY9578
SENP7PIAS4Q8N2W9571

IntAct

22 interactions, top by confidence:

ABTypeScore
CBX5SENP7psi-mi:“MI:0915”(physical association)0.670
SENP7TRIM28psi-mi:“MI:0915”(physical association)0.560
DAXXTNRC18psi-mi:“MI:0914”(association)0.530
SENP7VIMpsi-mi:“MI:0915”(physical association)0.400
Ppsi-mi:“MI:0914”(association)0.350
CBX5ZNF568psi-mi:“MI:0914”(association)0.350
H2BC21SMCHD1psi-mi:“MI:0914”(association)0.350
ZCCHC10C1orf226psi-mi:“MI:0914”(association)0.350
DAXXSETD1Apsi-mi:“MI:0914”(association)0.350
SETDB2DHX16psi-mi:“MI:0914”(association)0.350
CBX3ZNF324psi-mi:“MI:0914”(association)0.350
DAXXpsi-mi:“MI:0914”(association)0.350
BCL6CACNA1Apsi-mi:“MI:0914”(association)0.350
CBX3MYL12Bpsi-mi:“MI:0914”(association)0.350
CBX5ZNF292psi-mi:“MI:0914”(association)0.350
SENP7MYL12Bpsi-mi:“MI:0914”(association)0.350
HNRNPCSBNO1psi-mi:“MI:2364”(proximity)0.270
RBM15ILVBLpsi-mi:“MI:2364”(proximity)0.270
ZRANB2SBNO1psi-mi:“MI:2364”(proximity)0.270
NPM1SBNO1psi-mi:“MI:2364”(proximity)0.270

BioGRID (41): SENP7 (Synthetic Lethality), SENP7 (Affinity Capture-MS), SENP7 (Affinity Capture-MS), SENP7 (Affinity Capture-MS), CSTA (Affinity Capture-MS), MYL12B (Affinity Capture-MS), RBBP4 (Affinity Capture-MS), TRIM28 (Affinity Capture-MS), AHDC1 (Affinity Capture-MS), CBX3 (Affinity Capture-MS), CBX5 (Affinity Capture-MS), CHAMP1 (Affinity Capture-MS), SENP7 (Affinity Capture-Western), SPOP (Affinity Capture-Western), SENP7 (Affinity Capture-RNA)

ESM2 similar proteins: A0JM80, A6H8Y1, A7MBJ2, D3ZF42, E9Q6J5, F4I700, F4J3S1, F4KCE9, F6QRE9, O04251, O82345, P23497, P46100, P48785, P48786, Q04996, Q05B65, Q0WTB8, Q13342, Q15361, Q32MZ4, Q3UZ39, Q3ZBR9, Q4QSC8, Q571C7, Q5H9K5, Q5RHP9, Q61687, Q66HF9, Q7YQM3, Q7YQM4, Q7Z5L2, Q8BJM3, Q8C4A5, Q8C9B9, Q8GZ87, Q8H991, Q8IW19, Q92576, Q940Y3

Diamond homologs: A7MBJ2, D3ZF42, O13769, O42957, Q02724, Q6P7W0, Q8BUH8, Q8GYL3, Q8L7S0, Q94F30, Q9BQF6, Q9GZR1, Q0WKV8, Q2PS26, Q8RWN0, O65278, P59110, Q09353, Q5R7K7, Q5RBB1, Q6NXL6, Q8WP32, Q91ZX6, Q96HI0, Q9EP97, Q9EQE1, Q9H4L4, Q9HC62, Q9P0U3, O13612, Q09275, Q23238

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic1
Likely pathogenic2
Uncertain significance98
Likely benign12
Benign5

Top pathogenic / likely-pathogenic (3)

Variant IDHGVSClassification
4072000NM_020654.5(SENP7):c.973C>T (p.Gln325Ter)Pathogenic
2501008NM_020654.5(SENP7):c.1474C>T (p.Gln492Ter)Likely pathogenic
3340479NM_020654.5(SENP7):c.3088C>T (p.Arg1030Trp)Likely pathogenic

SpliceAI

5067 predictions. Top by Δscore:

VariantEffectΔscore
3:101326078:ATCC:Aacceptor_loss1.0000
3:101326079:TC:Tacceptor_gain1.0000
3:101326079:TCCT:Tacceptor_loss1.0000
3:101326080:CC:Cacceptor_gain1.0000
3:101328473:CT:Cdonor_loss1.0000
3:101328473:CTTA:Cdonor_gain1.0000
3:101328474:TT:Tdonor_loss1.0000
3:101328475:TACT:Tdonor_loss1.0000
3:101328476:A:ACdonor_gain1.0000
3:101328476:AC:Adonor_loss1.0000
3:101328476:ACT:Adonor_gain1.0000
3:101328476:ACTCT:Adonor_gain1.0000
3:101328477:C:CAdonor_gain1.0000
3:101328477:CT:Cdonor_gain1.0000
3:101328477:CTC:Cdonor_gain1.0000
3:101328477:CTCT:Cdonor_gain1.0000
3:101328477:CTCTC:Cdonor_gain1.0000
3:101328543:TGGC:Tacceptor_gain1.0000
3:101328545:GCCTA:Gacceptor_loss1.0000
3:101328546:CC:Cacceptor_loss1.0000
3:101328546:CCTA:Cacceptor_gain1.0000
3:101328547:C:CCacceptor_gain1.0000
3:101328548:T:Cacceptor_loss1.0000
3:101328549:A:ACacceptor_gain1.0000
3:101328549:A:Cacceptor_gain1.0000
3:101328641:CCTA:Cdonor_loss1.0000
3:101328644:ACC:Adonor_loss1.0000
3:101328686:TACTC:Tacceptor_loss1.0000
3:101328687:ACTCT:Aacceptor_loss1.0000
3:101328688:CT:Cacceptor_gain1.0000

AlphaMissense

6919 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
3:101326033:A:CF1021L1.000
3:101326033:A:TF1021L1.000
3:101326034:A:GF1021S1.000
3:101326035:A:GF1021L1.000
3:101326038:A:GW1020R1.000
3:101326038:A:TW1020R1.000
3:101327691:A:GL997S1.000
3:101327703:C:TG993E1.000
3:101327704:C:GG993R1.000
3:101327704:C:TG993R1.000
3:101327705:A:CC992W1.000
3:101327706:C:TC992Y1.000
3:101327707:A:GC992R1.000
3:101327723:C:AQ986H1.000
3:101327723:C:GQ986H1.000
3:101327733:A:TV983D1.000
3:101328481:C:GR954P1.000
3:101328526:T:AD939V1.000
3:101328535:A:GL936P1.000
3:101332089:A:TV865D1.000
3:101332100:C:AW861C1.000
3:101332100:C:GW861C1.000
3:101332102:A:GW861R1.000
3:101332102:A:TW861R1.000
3:101332105:G:CH860D1.000
3:101332826:C:AW839C1.000
3:101332826:C:GW839C1.000
3:101332828:A:GW839R1.000
3:101332828:A:TW839R1.000
3:101337574:A:CS805R1.000

dbSNP variants (sampled 300 via entrez): RS1000000241 (3:101476277 G>A), RS1000000322 (3:101387696 C>A,T), RS1000009165 (3:101432613 G>A), RS1000015585 (3:101339004 T>G), RS1000024397 (3:101513342 T>C), RS1000040786 (3:101395145 C>G), RS1000053372 (3:101374534 T>C), RS1000100321 (3:101483368 C>T), RS1000158959 (3:101495305 T>C), RS1000179356 (3:101438868 C>T), RS1000182907 (3:101473534 T>C), RS1000194688 (3:101346248 A>G), RS1000196503 (3:101395287 G>A), RS1000212696 (3:101452591 C>G), RS1000234625 (3:101445983 A>G)

Disease associations

OMIM: gene MIM:612846 | disease phenotypes:

GenCC curated gene-disease

DiseaseClassificationInheritance
arthrogryposis multiplex congenitaStrongAutosomal recessive

Mondo (1): arthrogryposis multiplex congenita (MONDO:0015168)

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

16 associations (top):

StudyTraitp-value
GCST004131_6Inflammatory bowel disease3.000000e-08
GCST004132_78Crohn’s disease4.000000e-07
GCST004630_120Mean corpuscular hemoglobin2.000000e-09
GCST007268_71Diastolic blood pressure9.000000e-13
GCST007511_24Alzheimer’s disease (late onset)4.000000e-06
GCST008522_94Bitter alcoholic beverage consumption8.000000e-06
GCST009066_33Mosaic loss of chromosome Y (Y chromosome dosage)8.000000e-19
GCST009067_24Mosaic loss of chromosome Y (Y chromosome dosage)6.000000e-44
GCST009856_15Leukocyte telomere length2.000000e-08
GCST010043_112Asthma4.000000e-08
GCST90002400_365Plateletcrit2.000000e-12
GCST90002403_548Red blood cell count5.000000e-13
GCST90011900_21Serum alkaline phosphatase levels2.000000e-10
GCST90013406_240Liver enzyme levels (alkaline phosphatase)2.000000e-20
GCST90020025_585Waist-to-hip ratio adjusted for BMI1.000000e-08
GCST90020027_362Waist-hip index5.000000e-09

EFO canonical traits (9, from GWAS)

EFO IDTrait name
EFO:0004527mean corpuscular hemoglobin
EFO:0006336diastolic blood pressure
EFO:1001870late-onset Alzheimers disease
EFO:0010092bitter alcoholic beverage consumption measurement
EFO:0007783mosaic loss of chromosome Y measurement
EFO:0007985platelet crit
EFO:0004305erythrocyte count
EFO:0004533alkaline phosphatase measurement
EFO:0007788BMI-adjusted waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1741213 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 5,477 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL165790IPRIFLAVONE25,477

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — C48: Ulp1 endopeptidase

Binding affinities (BindingDB)

8 measured of 18 human assays (18 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
SPI-02IC502100 nMUS-9791447: Methods of identifying SENP1 inhibitors
SPI-04IC502400 nMUS-9791447: Methods of identifying SENP1 inhibitors
SPI-10IC502400 nMUS-9791447: Methods of identifying SENP1 inhibitors
NSC8676IC503800 nMUS-9791447: Methods of identifying SENP1 inhibitors
NSC70551IC503900 nMUS-9791447: Methods of identifying SENP1 inhibitors
SPI-01IC505900 nMUS-9791447: Methods of identifying SENP1 inhibitors
SPI-05IC5013300 nMUS-9791447: Methods of identifying SENP1 inhibitors
SPI-08IC5022200 nMUS-9791447: Methods of identifying SENP1 inhibitors

ChEMBL bioactivities

670 potent at pChembl≥5 of 900 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.45IC50359nMCHEMBL3196451
6.31IC50490nMCHEMBL1870914
6.31IC50490nMCHEMBL1316867
6.25IC50558nMCHEMBL1870914
6.23IC50589nMCHEMBL1316867
6.20IC50635nMCHEMBL1525161
6.16IC50696nMCHEMBL281980
6.12IC50757nMCHEMBL3191962
6.12IC50750nMCHEMBL1402456
6.12IC50750nMCHEMBL1891588
6.10IC50788nMCHEMBL1421255
6.10IC50797nMCHEMBL1506796
6.07IC50857nMCHEMBL1542328
6.07IC50854nMCHEMBL1879394
6.06IC50863nMCHEMBL1967857
6.05IC50890nMCHEMBL1891206
6.05IC50896nMCHEMBL1586985
6.04IC50920nMCHEMBL1871228
6.04IC50910nMCHEMBL1884442
6.03IC50938nMCHEMBL1475128
6.02IC50955nMCHEMBL1418096
6.02IC50960nMCHEMBL1869393
6.01IC50987nMCHEMBL1871228
6.01IC50985nMCHEMBL1869875
6.00IC501010nMCHEMBL3195102
6.00IC501000nMCHEMBL1302779
6.00IC501000nMCHEMBL1319405
5.99IC501020nMCHEMBL1449923
5.97IC501060nMCHEMBL1889650
5.96IC501100nMCHEMBL1577231
5.96IC501100nMCHEMBL1878061
5.96IC501100nMCHEMBL1884495
5.94IC501140nMCHEMBL595840
5.94IC501160nMCHEMBL1869393
5.92IC501210nMCHEMBL1891206
5.92IC501200nMCHEMBL1877777
5.91IC501220nMCHEMBL1988780
5.91IC501230nMCHEMBL1302779
5.89IC501300nMCHEMBL1885269
5.88IC501310nMCHEMBL1773702
5.88IC501310nMCHEMBL1412015
5.87IC501360nMCHEMBL1417815
5.87IC501350nMCHEMBL1577231
5.87IC501360nMCHEMBL1319405
5.87IC501350nMCHEMBL1582654
5.86IC501390nMCHEMBL1877777
5.85IC501400nMCHEMBL1866613
5.85IC501400nMCHEMBL1890591
5.85IC501400nMCHEMBL1901952
5.84IC501460nMCHEMBL1521051

PubChem BioAssay actives

2 with measured affinity, of 9 total; 2 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
3-amino-4-[[4-[4-[(2-amino-6-sulfonaphthalen-1-yl)diazenyl]-3-methylphenyl]-2-methylphenyl]diazenyl]naphthalene-2,7-disulfonic acid1859347: Inhibition of His-tagged human SENP7 expressed in Escherichia coli (DE3) using YFP-SUMO-ECFP as substrate incubated for 15 mins by Coomassie staining based SDS-PAGE analysisic502.7000uM
[3-[[2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[2-(4-hydroxy-3-nitrophenyl)acetyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]acetyl]amino]-2-oxopropyl] anthracene-9-carboxylate1799555: Fluorogenic Assay from Article 10.1016/j.chembiol.2011.05.008: “Development of small molecule inhibitors and probes of human SUMO deconjugating proteases.”ic504.3000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects expression, affects methylation, decreases expression5
sodium arseniteincreases expression, decreases expression, affects cotreatment, increases abundance4
perfluorooctane sulfonic aciddecreases expression2
entinostatdecreases expression, affects cotreatment2
Arsenicdecreases expression, affects cotreatment, increases abundance2
Valproic Aciddecreases expression2
aristolochic acid Idecreases expression1
FR900359decreases phosphorylation1
dicrotophosdecreases expression1
methylmercuric chloridedecreases expression1
manganese chlorideaffects cotreatment, decreases expression, increases abundance1
potassium chromate(VI)affects cotreatment, decreases expression1
epigallocatechin gallateaffects cotreatment, decreases expression1
pentanaldecreases expression1
di-n-butylphosphoric acidaffects expression1
chromium hexavalent iondecreases expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamidedecreases expression, affects cotreatment1
abrineincreases expression1
dorsomorphinaffects cotreatment, decreases expression1
jinfukangaffects cotreatment, decreases expression1
Resveratrolaffects cotreatment, increases expression1
Sunitinibincreases expression1
Acetaminophendecreases expression1
Cisplatinaffects cotreatment, decreases expression1
Clorgylineincreases expression1
Doxorubicindecreases expression1
Estradiolaffects expression1
Folic Aciddecreases expression1
Manganesedecreases expression, increases abundance, affects cotreatment1
Methyl Methanesulfonateincreases expression1

ChEMBL screening assays

6 unique, capped per target: 3 functional, 3 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1738495FunctionalPUBCHEM_BIOASSAY: Dose Response confirmation of uHTS for inhibitors of Sentrin-specific protease 7 (SENP7) using a Luminescent assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID434973, AID434986]PubChem BioAssay data set
CHEMBL5114417BindingInhibition of His-tagged human SENP7 expressed in Escherichia coli (DE3) using YFP-SUMO-ECFP as substrate incubated for 15 mins by Coomassie staining based SDS-PAGE analysisSmall-molecule inhibitors targeting small ubiquitin-like modifier pathway for the treatment of cancers and other diseases. — Eur J Med Chem

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

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

CellosaurusNameCategorySex
CVCL_E1C7Ubigene SK-BR-3 SENP7 KOCancer cell lineFemale
CVCL_E2JSHAP1 SENP7 (-) 2Cancer cell lineMale
CVCL_E2JTHAP1 SENP7 (-) 3Cancer cell lineMale
CVCL_XS56HAP1 SENP7 (-) 1Cancer cell lineMale

Clinical trials (associated diseases)

4 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT05393375Not specifiedCOMPLETEDArthrogryposis Multiplex Congenita in Pediatric Age: Correlation Between MUScular MRI and Functional Evaluation
NCT05673265Not specifiedUNKNOWNPediatric and Adult Registry for Patients With ARThrogryposis
NCT06130592Not specifiedUNKNOWNTechnical Feasibility Study of Ultrasound Muscle Imaging in Antenatal Ultrasound
NCT07360574Not specifiedNOT_YET_RECRUITINGPiezo2-related Arthrogryposis & physiopathOLOgy 3