DGIdb - TSPO Gene Record

TSPO 706 Druggable Genome

Alternate Names:

706
TRANSLOCATOR PROTEIN
TSPO
BPBS
BZRP
DBI
IBP
MBR
PBR
PBS
PKBS
PTBR
mDRC
pk18
109610
1158
ENSG00000100300
OTTHUMG00000150573
P30536
PERIPHERAL-TYPE BENZODIAZEPINE RECEPTOR (PBR) (PKBS) (MITOCHONDRIAL BENZODIAZEPINE RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30536]
TSPOA_HUMAN
T75440

Gene Info:

Human Readable Name	DRUGGABLE GENOME
Transmembrane Helix Count	5
Target Subclass	Other
Target Main Class	Transporters
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	TspO_MBR
Interpro Name	TspO/MBR-related protein
Interpro Type	Family
Interpro Acc	IPR004307
Target Class	Transporters
Target Subclass	Miscellaneous
Target Subclass	benzodiazepine translocator protein,
Gene Biotype	PROTEIN_CODING

(4 More Sources)

Gene Categories: Category Details

DRUGGABLE GENOME

Publications:

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Rupprecht R et al., 2010, Translocator protein (18 kDa) (TSPO) as a therapeutic target for neurological and psychiatric disorders., Nat Rev Drug Discov
Falchi et al., 2007, Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands., Neuropharmacology
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Miller et al., 2006, Detection of benzodiazepines in hair using ELISA and LC-ESI-MS-MS., J Anal Toxicol
Dobbin et al., 2003, Association of benzodiazepine injection with the prescription of temazepam capsules., Drug Alcohol Rev
Mant et al., 1993, Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database., Aust J Public Health
Becker et al., 2009, Treatment of sleep dysfunction and psychiatric disorders., Curr Treat Options Neurol
Jufe, [New hypnotics: perspectives from sleep physiology]., Vertex
Park et al., 1996, Characterization of peripheral benzodiazepine type sites in a cultured murine BV-2 microglial cell line., Glia
Katz et al., 1992, Disulfiram and diethyldithiocarbamate are competitive inhibitors at the peripheral benzodiazepine receptor., J. Pharmacol. Exp. Ther.
Venneti et al., 2006, The peripheral benzodiazepine receptor (Translocator protein 18kDa) in microglia: from pathology to imaging., Prog. Neurobiol.
Uusi-Oukari et al., 1991, Specific alterations in the cerebellar GABA(A) receptors of an alcohol-sensitive ANT rat line., Alcohol. Clin. Exp. Res.
Poisnel et al., 2009, Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation., J. Pharmacol. Sci.
Papadopoulos et al., 1991, Diazepam binding inhibitor and its processing products stimulate mitochondrial steroid biosynthesis via an interaction with mitochondrial benzodiazepine receptors., Endocrinology
Awad et al., 1989, Solubilization of peripheral-type benzodiazepine binding sites from cat cerebral cortex., J. Neurochem.
Gandolfo et al., 1997, The stimulatory effect of the octadecaneuropeptide (ODN) on cytosolic Ca2+ in rat astrocytes is not mediated through classical benzodiazepine receptors., Eur. J. Pharmacol.
Papadopoulos et al., 1991, Hormone-stimulated steroidogenesis is coupled to mitochondrial benzodiazepine receptors. Tropic hormone action on steroid biosynthesis is inhibited by flunitrazepam., J. Biol. Chem.
Carmel et al., 1999, Peripheral-type benzodiazepine receptors in the regulation of proliferation of MCF-7 human breast carcinoma cell line., Biochem. Pharmacol.
Bono et al., 1999, Peripheral benzodiazepine receptor agonists exhibit potent antiapoptotic activities., Biochem. Biophys. Res. Commun.
Marano et al., 1990, Enhancement of pharmacologically induced bronchoconstriction by Ro 5-4864., Eur. J. Pharmacol.
Bolger et al., 1990, Interactions between peripheral-type benzodiazepine receptor ligands and an activator of voltage-operated calcium channels., Can. J. Physiol. Pharmacol.
Campagna et al., 2004, Synthesis, central and peripheral benzodiazepine receptor affinity of pyrazole and pyrazole-containing polycyclic derivatives., Farmaco

CHLORMEZANONE TSPO

Interaction Score: 10.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD
DIAZEPINOMICIN TSPO

Interaction Score: 3.64

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name TLN-4601, ECO-4601

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
FLUNITRAZEPAM TSPO

Interaction Score: 2.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19443999 1320691 1651852 2723642 9098698 1847384

Sources:
TdgClinicalTrial TEND TTD
ALPIDEM TSPO

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ONO-2952 TSPO

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DEXTOFISOPAM TSPO

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ZOPICLONE TSPO

Interaction Score: 1.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 21119734

Sources:
TdgClinicalTrial TEND
ZALEPLON TSPO

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AZ-007, Staccato zaleplon

Novel drug target Established target

Trial Name SKP-1041, delayed-release zaleplon

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
PYRAZOLE TSPO

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15544788

Sources:
NCI
METRONIDAZOLE TSPO

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1320691

Sources:
NCI
ESZOPICLONE TSPO

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

PMIDs:
19744401 18265473 17016423 17139284

Sources:
TdgClinicalTrial TTD
LORAZEPAM TSPO

Interaction Score: 0.58

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17156911 1647706 16959136 8787774

Sources:
TdgClinicalTrial TEND TTD
CLONAZEPAM TSPO

Interaction Score: 0.55

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10423168 10558889 2364987 2723642 1691678 11752352

Sources:
TEND
TEMAZEPAM TSPO

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16959136 12850901 7911332

Sources:
TdgClinicalTrial TEND TTD
OLESOXIME TSPO

Interaction Score: 0.45

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name olesoxime, TRO19622

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
CLORAZEPIC ACID TSPO

Interaction Score: 0.36

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8787774

Sources:
TdgClinicalTrial TEND TTD
DIAZEPAM TSPO

Interaction Score: 0.24

Interaction Types & Directionality:

potentiator

Interaction Info:

PMIDs:
17631921 11752352

Sources:
TEND TTD
ZOLPIDEM TSPO

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
TRIAZOLAM TSPO

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8787774

Sources:
TEND TTD
ALPRAZOLAM TSPO

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND TTD
FLUDIAZEPAM TSPO

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CINOLAZEPAM TSPO

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ADINAZOLAM TSPO

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CLOTIAZEPAM TSPO

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLUMAZENIL TSPO

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DISULFIRAM TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1320691

Sources:
NCI
HALAZEPAM TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
QUAZEPAM TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHLORDIAZEPOXIDE TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLURAZEPAM TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PRAZEPAM TSPO

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ESTAZOLAM TSPO

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
OXAZEPAM TSPO

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MIDAZOLAM TSPO

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD

Ensembl: ENSG00000100300
- Version: 101_38
Alternate Names:

TSPO Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P30536
- Version: 01-August-2011
Alternate Names:

TSPOA_HUMAN Uniprot Id

706 Entrez Gene Id

BZRP Gene Symbol

Gene Info:

Transmembrane Helix Count 5

Target Subclass Other

Target Main Class Transporters

Publications:
TdgClinicalTrial: P30536
- Version: January-2014
Alternate Names:

TSPO Gene Symbol

BZRP Gene Symbol

Gene Info:

Target Class Transporters

Target Subclass Miscellaneous

Target Subclass benzodiazepine translocator protein,

Publications:

RussLampel: ENSG00000100300

Version: 26-July-2011

Alternate Names:

PERIPHERAL-TYPE BENZODIAZEPINE RECEPTOR (PBR) (PKBS) (MITOCHONDRIAL BENZODIAZEPINE RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30536] Description

BZRP Display Id

ENSG00000100300 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P30536
- Version: 11-September-2012
Alternate Names:

TRANSLOCATOR PROTEIN Uniprot Protein Name

706 Entrez Gene Id

TSPO Uniprot Gene Name

Gene Info:

Uniprot Status Swiss-Prot

Uniprot Evidence 1: Evidence at protein level

Interpro Short Name TspO_MBR

Gene Categories:

DRUGGABLE GENOME

Publications:

NCI: TSPO

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Katz et al., 1992, Disulfiram and diethyldithiocarbamate are competitive inhibitors at the peripheral benzodiazepine receptor., J. Pharmacol. Exp. Ther.

Campagna et al., 2004, Synthesis, central and peripheral benzodiazepine receptor affinity of pyrazole and pyrazole-containing polycyclic derivatives., Farmaco

HingoraniCasas: ENSG00000100300
- Version: 31-May-2017
Alternate Names:

ENSG00000100300 Gene Symbol

TSPO Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TTD: Translocator protein
- Version: 2020.06.01
Alternate Names:

TSPO TTD Gene Abbreviation

T75440 TTD Target ID

Gene Info:

Publications:

Trial Name	TLN-4601, ECO-4601
Novel drug target	Established target

Trial Name	AZ-007, Staccato zaleplon
Novel drug target	Established target
Trial Name	SKP-1041, delayed-release zaleplon

Trial Name	olesoxime, TRO19622
Novel drug target	Established target

PERIPHERAL-TYPE BENZODIAZEPINE RECEPTOR (PBR) (PKBS) (MITOCHONDRIAL BENZODIAZEPINE RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P30536]	Description
BZRP	Display Id
ENSG00000100300	Ensembl Gene Id

TRANSLOCATOR PROTEIN	Uniprot Protein Name
706	Entrez Gene Id
TSPO	Uniprot Gene Name

TSPO Gene Record

TSPO 706 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name TLN-4601, ECO-4601 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 19443999 1320691 1651852 2723642 9098698 1847384

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 21119734

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info: Trial Name AZ-007, Staccato zaleplon Novel drug target Established target Trial Name SKP-1041, delayed-release zaleplon

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15544788

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1320691

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name Lunesta

PMIDs: 19744401 18265473 17016423 17139284

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17156911 1647706 16959136 8787774

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10423168 10558889 2364987 2723642 1691678 11752352

Sources: TEND

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 16959136 12850901 7911332

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name olesoxime, TRO19622 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8787774

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: potentiator

Interaction Info:

PMIDs: 17631921 11752352

Sources: TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TEND

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name TLN-4601, ECO-4601

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19443999 1320691 1651852 2723642 9098698 1847384

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 21119734

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AZ-007, Staccato zaleplon

Novel drug target Established target

Trial Name SKP-1041, delayed-release zaleplon

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
15544788

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1320691

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

PMIDs:
19744401 18265473 17016423 17139284

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17156911 1647706 16959136 8787774

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
10423168 10558889 2364987 2723642 1691678 11752352

Sources:
TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16959136 12850901 7911332

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name olesoxime, TRO19622

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8787774

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

potentiator

PMIDs:
17631921 11752352

Sources:
TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND

Interaction Types & Directionality:

n/a

PMIDs:
8787774

Sources:
TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a