TSPO
gene geneOn this page
Also known as PBRMBRPKBSmDRCDBIIBPpk18TSPO1
Summary
TSPO (translocator protein, HGNC:1158) is a protein-coding gene on chromosome 22q13.2, encoding Putative peripheral benzodiazepine receptor-related protein (B1AH88).
Present mainly in the mitochondrial compartment of peripheral tissues, the protein encoded by this gene interacts with some benzodiazepines and has different affinities than its endogenous counterpart. The protein is a key factor in the flow of cholesterol into mitochondria to permit the initiation of steroid hormone synthesis. Alternatively spliced transcript variants have been reported; one of the variants lacks an internal exon and is considered non-coding, and the other variants encode the same protein.
Source: NCBI Gene 706 — RefSeq curated summary.
At a glance
- GWAS associations: 6
- Clinical variants (ClinVar): 24 total
- Druggable target: yes
- MANE Select transcript:
NM_000714
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1158 |
| Approved symbol | TSPO |
| Name | translocator protein |
| Location | 22q13.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PBR, MBR, PKBS, mDRC, DBI, IBP, pk18, TSPO1 |
| Ensembl gene | ENSG00000100300 |
| Ensembl biotype | protein_coding |
| OMIM | 109610 |
| Entrez | 706 |
Gene structure
Transcript identifiers
Ensembl transcripts: 24 — 23 protein_coding, 1 retained_intron
ENST00000329563, ENST00000337554, ENST00000396265, ENST00000428336, ENST00000472378, ENST00000583777, ENST00000864330, ENST00000864331, ENST00000864332, ENST00000864333, ENST00000864334, ENST00000864335, ENST00000864336, ENST00000864337, ENST00000864338, ENST00000864339, ENST00000864340, ENST00000864341, ENST00000864342, ENST00000924335, ENST00000972386, ENST00000972387, ENST00000972388, ENST00000972389
RefSeq mRNA: 3 — MANE Select: NM_000714
NM_000714, NM_001256530, NM_001256531
CCDS: CCDS33661
Canonical transcript exons
ENST00000337554 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001106768 | 43151559 | 43151604 |
| ENSE00001708696 | 43162803 | 43163242 |
| ENSE00002316005 | 43159210 | 43159420 |
| ENSE00003788871 | 43161052 | 43161190 |
Expression profiles
Bgee: expression breadth ubiquitous, 271 present calls, max score 99.42.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 96.2500 / max 1685.7732, expressed in 1757 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 192593 | 93.1008 | 1756 |
| 192594 | 1.2321 | 776 |
| 192595 | 0.4442 | 266 |
| 192600 | 0.3810 | 182 |
| 192597 | 0.3690 | 194 |
| 192598 | 0.3453 | 170 |
| 192596 | 0.2195 | 73 |
| 192599 | 0.1580 | 51 |
Top tissues by expression
290 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| lower esophagus mucosa | UBERON:0035834 | 99.42 | gold quality |
| esophagus mucosa | UBERON:0002469 | 99.32 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 99.26 | gold quality |
| gingival epithelium | UBERON:0001949 | 99.23 | gold quality |
| granulocyte | CL:0000094 | 99.21 | gold quality |
| monocyte | CL:0000576 | 99.21 | gold quality |
| skin of abdomen | UBERON:0001416 | 99.20 | gold quality |
| mononuclear cell | CL:0000842 | 99.15 | gold quality |
| leukocyte | CL:0000738 | 99.14 | gold quality |
| gingiva | UBERON:0001828 | 99.14 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 99.13 | gold quality |
| skin of leg | UBERON:0001511 | 99.12 | gold quality |
| mouth mucosa | UBERON:0003729 | 98.82 | gold quality |
| minor salivary gland | UBERON:0001830 | 98.78 | gold quality |
| zone of skin | UBERON:0000014 | 98.72 | gold quality |
| nipple | UBERON:0002030 | 98.67 | gold quality |
| left coronary artery | UBERON:0001626 | 98.66 | gold quality |
| body of stomach | UBERON:0001161 | 98.65 | gold quality |
| ascending aorta | UBERON:0001496 | 98.55 | gold quality |
| thoracic aorta | UBERON:0001515 | 98.55 | gold quality |
| bone marrow | UBERON:0002371 | 98.54 | gold quality |
| coronary artery | UBERON:0001621 | 98.53 | gold quality |
| omental fat pad | UBERON:0010414 | 98.52 | gold quality |
| penis | UBERON:0000989 | 98.51 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 98.49 | gold quality |
| peritoneum | UBERON:0002358 | 98.49 | gold quality |
| right coronary artery | UBERON:0001625 | 98.48 | gold quality |
| upper leg skin | UBERON:0004262 | 98.46 | gold quality |
| right lung | UBERON:0002167 | 98.45 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 98.42 | gold quality |
Single-cell (SCXA)
Detected in 29 experiment(s), a significant marker in 23.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10042 | yes | 3248.91 |
| E-CURD-112 | yes | 1694.14 |
| E-HCAD-4 | yes | 320.36 |
| E-HCAD-1 | yes | 247.19 |
| E-CURD-122 | yes | 90.41 |
| E-GEOD-125970 | yes | 48.26 |
| E-HCAD-6 | yes | 45.82 |
| E-MTAB-8410 | yes | 45.80 |
| E-HCAD-10 | yes | 41.33 |
| E-MTAB-6701 | yes | 40.62 |
| E-MTAB-9467 | yes | 38.69 |
| E-MTAB-9221 | yes | 27.91 |
| E-HCAD-9 | yes | 26.34 |
| E-GEOD-130148 | yes | 26.22 |
| E-GEOD-134144 | yes | 25.41 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AP1, IRF4, JUN, MYC, PPARA, SP1, SP3, SP4, SPI1, STAT3, TCF3, TP53
Literature-anchored findings (GeneRIF, showing 40)
- Overexpression of the peripheral benzodiazepine receptor is associated with colorectal cancer (PMID:12374690)
- This gene is amplified in MDA-MB-231 aggressive breast cancer cells (PMID:12547158)
- demonstrated that PBR is expressed in mesenchymal stem cells and that their ligands affect their proliferation and differentiation (PMID:14584048)
- These results indicate that elevated peripheral-type benzodiazepine receptor (PBR) expression is not common in aggressive tumors, but may be limited to certain cancers where elevated PBR expression is associated with tumor progression. (PMID:14626449)
- High expression of PBR in this patient subgroup may be used to identify a new high risk population in breast cancer for which a more specific therapy would be beneficial. (PMID:15041726)
- involvement of PBRs in human pancreatic beta-cell function and survival. (PMID:15296476)
- our results supported the hypothesis that PBR controls T-cell maturation and suggested mechanisms through which PBR may regulate thymocyte-positive selection. (PMID:15473257)
- Our results represent first evidence of PBRs in parathyroid glands and suggest for them a role in influencing PTH release. A clear trend of PBR up-regulation in parathyroid adenoma was also found. (PMID:15648546)
- the subcellular localisation of PBR defines its function and that this receptor could be a possible target for new strategies against cancer (PMID:15769477)
- Study provides new and important evidence that variation in the PBR gene influences susceptibility to panic disorder. (PMID:16511838)
- the intensity and extent of staining for PBR had a strong direct correlation with the grade of malignancy of the tumor, along with proliferative and apoptotic indices. The highest expression of PBR was in glioblastomas grade IV. (PMID:16868661)
- Our results showed an up-regulation of peripheral-type benzodiazepine receptor (PBR) in platelets of FM patients, and this seems to be related to the severity of fibromyalgic symptoms. (PMID:16919618)
- TSPO is located in mitochondrial membranes of HT-29 and reveal that its activation induces a rise in cytosolic Ca(2+), leading to the stimulation of Cl(-) secretion. (PMID:17561806)
- TSPO expression evaluation is a useful biological marker of Adult Separation Anxiety Disorder (PMID:18054208)
- These findings reveal a previously unidentified pathway of the membrane integration of MOM proteins with multiple TMSs of the PBR. (PMID:18158327)
- Sharp inhibition of apoptosis and changes in the levels of cell proliferation in tumor cells were paralleled by decreased expression of peripheral benzodiazepine receptor in patients with squamous cell carcinoma & skin melanoma. (PMID:18256758)
- VDAC activation by the 18 kDa translocator protein (TSPO), implications for apoptosis. (PMID:18670869)
- TSPO may serve to open the mitochondrial permeability transition pore in response to anti-cancer drugs such as erucylphosphohomocholine (PMID:18791274)
- TSPO knockdown by genetic manipulation transforms the human HT29 cancer line to a more malignant type in-vitro. (PMID:18806692)
- results show variety of CNS cells capable of expressing TSPO; pattern of expression differs between normal & diseased CNS & among different diseases & cell types; microglia & macrophages remain chief cell type upregulating TSPO expression in brain disease (PMID:19077109)
- (11)C-AC-5216 is a promising PET ligand for quantifying PBR in the human brain. (PMID:19525461)
- (18)F-PBR06 is a longer-lived and promising alternative to (11)C-labeled radioligands to measure TSPOs as a biomarker of inflammation in the brain. (PMID:19525468)
- Studies in patient populations will help determine whether (11)C-DPA-713 provides better sensitivity for evaluating increased TSPO expression. (PMID:19617321)
- Two allelic variants of TSPO gene, were tested for association with the presence of adult separation anxiety disorder. (PMID:19668118)
- Blocking TSPO function in tumor cells induces cell death and denotes a survival role for TSPO in prostate cancer . (PMID:19789311)
- Results demonstrate that the Ala147Thr spontaneous amino acid substitution within TSPO is able to affect pregnenolone production, and should encourage further studies to investigate its potential role in polygenic dyslipidemias. (PMID:19846611)
- TSPO is expressed in macrophages in human carotid atherosclerosis (PMID:20056222)
- High TSPO protein levels are associated with oral cancer. (PMID:20085808)
- Overexpression of translocator protein is associated with inflammatory bowel disease. (PMID:20222126)
- reduction in [(11)C]PBR28 binding may not be interpreted simply as a reduction in TSPO density (PMID:20424634)
- Following exposure of saliva to cigarette smoke a three-fold decrease in the affinity of salivary TSPO to its specific ligand, [(3)H]PK 11195 (p < 0.01) occurred in the cellular fraction of the saliva. (PMID:20491643)
- This review focuses on the current knowledge regarding the chemicals, hormones, and molecular mechanisms regulating Tspo gene expression under physiological conditions in a tissue- and disease-specific manner. (PMID:20600583)
- These results further define TSPO as an informative marker of glial activation in multiple sclerosis (PMID:20872081)
- The present data indicate that [(11)C]vinpocetine may serve as a molecular imaging biomarker of the activity of the TSPO system (PMID:21320609)
- The translocator protein. (PMID:21498529)
- these experiments constitute the first in-depth functional analysis of the human TSPO gene promoter and its transcriptional regulation (PMID:21958735)
- An 18-kDa Translocator Protein polymorphism explains differences in binding affinity of the PET radioligand PBR28. (PMID:22008728)
- This review describes the principles of positron emission tomography (PET) imaging, the rationale and challenges in targeting the TSPO as a means of quantifying microglial activation in vivo. (PMID:22050847)
- PK 11195 exerted a suppressive effect on VDAC1 and caused an increase in TSPO gene expression or protein levels. (PMID:22127435)
- increased expression of TSPO in temporal lobe epilepsy (PMID:22238156)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Tspo | ENSMUSG00000041736 |
| rattus_norvegicus | Tspo | ENSRNOG00000010549 |
| drosophila_melanogaster | Tspo | FBGN0031263 |
| caenorhabditis_elegans | tspo-1 | WBGENE00077771 |
Paralogs (1): TSPO2 (ENSG00000112212)
Protein
Protein identifiers
Putative peripheral benzodiazepine receptor-related protein — B1AH88 (reviewed: B1AH88, P30536)
All UniProt accessions (3): P30536, B1AH87, J3QLD3
UniProt curated annotations — full annotation on UniProt →
Tissue specificity. Ubiquitous.
Miscellaneous. The relatively low levels of the corresponding mRNA suggest that it might represent errors of the splicing machinery. In addition, isoform 2 is derived from a different reading frame, compared to isoform 1 and lacks homolog support.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| B1AH88-1 | 2, PBR-S | yes |
| P30536-1 | 1 |
RefSeq proteins (3): NP_000705, NP_001243459, NP_001243460 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004307 | TspO_MBR | Family |
| IPR038330 | TspO/MBR-related_sf | Homologous_superfamily |
Pfam: PF03073
UniProt features (19 total): topological domain 6, transmembrane region 5, sequence variant 4, chain 2, sequence conflict 1, initiator methionine 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-B1AH88-F1 | 44.67 | 0.00 |
| AF-P30536-F1 | 66.34 | 0.00 |
Function
Pathways and Gene Ontology
Reactome pathways
1 pathways
| ID | Pathway |
|---|---|
| R-HSA-196108 | Pregnenolone biosynthesis |
MSigDB gene sets: 733 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_DN, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, BORCZUK_MALIGNANT_MESOTHELIOMA_UP, GOBP_REGULATION_OF_AUTOPHAGY, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, GOBP_RESPONSE_TO_ZINC_ION, GOBP_BEHAVIOR, GOBP_STEROL_HOMEOSTASIS, GOBP_CELLULAR_RESPONSE_TO_LIPID
GO Biological Process (45): obsolete protein targeting to mitochondrion (GO:0006626), C21-steroid hormone biosynthetic process (GO:0006700), heme biosynthetic process (GO:0006783), monoatomic anion transport (GO:0006820), chloride transport (GO:0006821), steroid metabolic process (GO:0008202), glial cell migration (GO:0008347), response to xenobiotic stimulus (GO:0009410), response to manganese ion (GO:0010042), response to vitamin B1 (GO:0010266), peripheral nervous system axon regeneration (GO:0014012), adrenal gland development (GO:0030325), negative regulation of protein ubiquitination (GO:0031397), regulation of cholesterol transport (GO:0032374), response to progesterone (GO:0032570), negative regulation of tumor necrosis factor production (GO:0032720), response to testosterone (GO:0033574), regulation of cell population proliferation (GO:0042127), cholesterol homeostasis (GO:0042632), positive regulation of apoptotic process (GO:0043065), negative regulation of nitric oxide biosynthetic process (GO:0045019), behavioral response to pain (GO:0048266), regulation of steroid biosynthetic process (GO:0050810), positive regulation of mitochondrial depolarization (GO:0051901), positive regulation of calcium ion transport (GO:0051928), contact inhibition (GO:0060242), positive regulation of glial cell proliferation (GO:0060252), negative regulation of glial cell proliferation (GO:0060253), positive regulation of programmed necrotic cell death (GO:0062100), cellular response to lipopolysaccharide (GO:0071222), cellular response to zinc ion (GO:0071294), cellular hypotonic response (GO:0071476), maintenance of protein location in mitochondrion (GO:0072656), negative regulation of mitophagy (GO:1901525), negative regulation of ATP metabolic process (GO:1903579), response to acetylcholine (GO:1905144), positive regulation of reactive oxygen species metabolic process (GO:2000379), negative regulation of corticosterone secretion (GO:2000853), steroid biosynthetic process (GO:0006694), monoatomic ion transport (GO:0006811)
GO Molecular Function (6): androgen binding (GO:0005497), benzodiazepine receptor activity (GO:0008503), cholesterol binding (GO:0015485), transmembrane transporter binding (GO:0044325), cholesterol transfer activity (GO:0120020), protein binding (GO:0005515)
GO Cellular Component (6): mitochondrion (GO:0005739), mitochondrial outer membrane (GO:0005741), cytosol (GO:0005829), membrane (GO:0016020), extracellular exosome (GO:0070062), mitochondrial membrane (GO:0031966)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Metabolism of steroid hormones | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| response to ketone | 2 |
| cytoplasm | 2 |
| cellular anatomical structure | 2 |
| C21-steroid hormone metabolic process | 1 |
| hormone biosynthetic process | 1 |
| steroid hormone biosynthetic process | 1 |
| porphyrin-containing compound biosynthetic process | 1 |
| heme metabolic process | 1 |
| pigment biosynthetic process | 1 |
| monoatomic ion transport | 1 |
| monoatomic anion transport | 1 |
| inorganic anion transport | 1 |
| lipid metabolic process | 1 |
| cell migration | 1 |
| gliogenesis | 1 |
| response to chemical | 1 |
| response to metal ion | 1 |
| response to vitamin | 1 |
| response to alcohol | 1 |
| response to nitrogen compound | 1 |
| axon regeneration | 1 |
| endocrine system development | 1 |
| gland development | 1 |
| protein ubiquitination | 1 |
| regulation of protein ubiquitination | 1 |
| negative regulation of protein modification by small protein conjugation or removal | 1 |
| cholesterol transport | 1 |
| regulation of sterol transport | 1 |
| response to steroid hormone | 1 |
| tumor necrosis factor production | 1 |
| regulation of tumor necrosis factor production | 1 |
| negative regulation of tumor necrosis factor superfamily cytokine production | 1 |
| response to lipid | 1 |
| cell population proliferation | 1 |
| regulation of cellular process | 1 |
| sterol homeostasis | 1 |
| apoptotic process | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of programmed cell death | 1 |
| hormone binding | 1 |
Protein interactions and networks
STRING
0 interactions, top by confidence (×1000):
IntAct
0 interactions, top by confidence:
ESM2 similar proteins: A0A1W2PPE3, A0A3B3IS91, A0A6I8MX38, A0A6I8PU40, A8MTW9, B1AH88, B3EWF7, C0HLS1, C0HMD6, H3BQW9, I3L0S3, I3L1E1, O70738, O75638, P03289, P0C880, P0DI83, P11300, P13985, P16807, P29164, P33485, P59091, P80612, Q01480, Q01900, Q3SYB3, Q5JLA7, Q5SY85, Q5T4H9, Q63003, Q6EEV4, Q6VB84, Q86SI9, Q8N1I8, Q8N1X5, Q8N319, Q8N6K4, Q8N6U2, Q8N726
SIGNOR signaling
0 interactions.
Disease & clinical
Cancer significance
Clinical variants and AI predictions
ClinVar
24 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 12 |
| Likely benign | 9 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1241 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 22:43161046:TTTCA:T | acceptor_loss | 1.0000 |
| 22:43161047:TTCAG:T | acceptor_loss | 1.0000 |
| 22:43161049:CA:C | acceptor_loss | 1.0000 |
| 22:43161050:A:AT | acceptor_loss | 1.0000 |
| 22:43161051:GGT:G | acceptor_gain | 1.0000 |
| 22:43161051:GGTAC:G | acceptor_gain | 1.0000 |
| 22:43161186:GCTGG:G | donor_gain | 1.0000 |
| 22:43161188:TGGGT:T | donor_loss | 1.0000 |
| 22:43161189:GG:G | donor_gain | 1.0000 |
| 22:43161189:GGGTA:G | donor_loss | 1.0000 |
| 22:43161190:GG:G | donor_gain | 1.0000 |
| 22:43161190:GGT:G | donor_loss | 1.0000 |
| 22:43161191:GT:G | donor_loss | 1.0000 |
| 22:43161192:T:TC | donor_loss | 1.0000 |
| 2:119368303:CAGG:C | donor_loss | 1.0000 |
| 2:119368304:AGG:A | donor_loss | 1.0000 |
| 2:119368305:GGTA:G | donor_loss | 1.0000 |
| 2:119368306:G:GC | donor_loss | 1.0000 |
| 2:119368307:T:G | donor_loss | 1.0000 |
| 2:119370737:A:AG | acceptor_gain | 1.0000 |
| 2:119370738:A:AG | acceptor_gain | 1.0000 |
| 2:119370739:G:GA | acceptor_gain | 1.0000 |
| 2:119370739:GAAC:G | acceptor_gain | 1.0000 |
| 2:119370801:AGG:A | donor_loss | 1.0000 |
| 2:119370803:G:A | donor_loss | 1.0000 |
| 2:119370804:T:A | donor_loss | 1.0000 |
| 22:43151601:GCTG:G | donor_gain | 0.9900 |
| 22:43151602:CTGGT:C | donor_loss | 0.9900 |
| 22:43151604:GGT:G | donor_loss | 0.9900 |
| 22:43151605:G:GG | donor_gain | 0.9900 |
AlphaMissense
0 scored. Top likely-pathogenic:
dbSNP variants (sampled 300 via entrez): RS1000068385 (22:43156907 A>G), RS1000072325 (22:43156897 T>C), RS1000206374 (22:43161823 T>C), RS1000402275 (22:43157031 G>A), RS1000496175 (22:43152642 G>A,C), RS1000695358 (22:43158058 C>A), RS1000907475 (22:43163593 C>T), RS1001568370 (22:43154435 T>G), RS1001879141 (22:43160320 T>A,C), RS1002150410 (22:43155671 C>G), RS1002502325 (22:43158439 C>A), RS1002505864 (22:43155297 G>A), RS1002574353 (22:43158223 A>G), RS1002610650 (22:43163671 C>A), RS1002702457 (22:43160362 T>C)
Disease associations
OMIM: gene MIM:109610 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
6 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004609_169 | Monocyte percentage of white cells | 1.000000e-12 |
| GCST004625_197 | Monocyte count | 4.000000e-22 |
| GCST009391_1949 | Metabolite levels | 3.000000e-06 |
| GCST90002393_593 | Monocyte count | 6.000000e-43 |
| GCST90002394_210 | Monocyte percentage of white cells | 6.000000e-26 |
| GCST90002407_376 | White blood cell count | 1.000000e-11 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007989 | monocyte percentage of leukocytes |
| EFO:0005091 | monocyte count |
| EFO:0010462 | aspartate measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5139 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
CTD chemical–gene interactions
69 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, increases expression, affects expression, decreases expression, increases methylation | 9 |
| trichostatin A | affects cotreatment, increases expression | 3 |
| sodium arsenite | decreases expression, increases expression | 3 |
| Particulate Matter | increases expression, decreases expression, increases abundance, affects cotreatment | 3 |
| methylmercuric chloride | decreases expression | 2 |
| chloropicrin | decreases expression | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| Panobinostat | affects cotreatment, increases expression | 2 |
| Air Pollutants | decreases expression, increases abundance | 2 |
| Ethanol | affects cotreatment, increases expression, increases abundance | 2 |
| Cisplatin | affects expression, affects cotreatment, increases expression | 2 |
| Tetrachlorodibenzodioxin | increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| bisphenol F | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| beta-lapachone | increases expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| mono-(2-ethylhexyl)phthalate | decreases expression, increases expression | 1 |
| cobaltous chloride | decreases expression | 1 |
| fluorotelomer alcohols | decreases expression | 1 |
| PK 11195 | affects binding | 1 |
| isobutyl alcohol | affects cotreatment, increases abundance, increases expression | 1 |
| perfluorooctane sulfonic acid | increases expression | 1 |
| SSR180575 | affects binding | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| ICG 001 | increases expression | 1 |
| N-benzyl-N-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9H-purin-9-yl)acetamide | affects binding | 1 |
| 2,2’,4,4’-tetrabromodiphenyl ether | decreases expression | 1 |
| pyrachlostrobin | decreases activity | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
ChEMBL screening assays
1 unique, capped per target: 1 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL6194625 | Binding | Binding affinity to hTSPO at compound concentration of 10.0 uM using Eurofins-Cerep binding assay | Data for DCP probe JNJ-78911118 |
Cellosaurus cell lines
6 cell lines: 6 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1EB | Abcam HCT 116 TSPO KO | Cancer cell line | Male |
| CVCL_B2JU | Abcam HeLa TSPO KO | Cancer cell line | Female |
| CVCL_D1UR | Abcam U-87MG TSPO KO | Cancer cell line | Male |
| CVCL_E0SE | Ubigene HeLa TSPO KO | Cancer cell line | Female |
| CVCL_TU95 | HAP1 TSPO (-) 1 | Cancer cell line | Male |
| CVCL_TU96 | HAP1 TSPO (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.