Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00454

Target Information
NamePeripheral-type benzodiazepine receptor    
Type of targetSuccessful target    
SynonymsMitochondrial benzodiazepine receptor    
PBR    
PKBS    
Peripheral benzodiazepine receptor    
Translocator protein    
DiseaseAngina pectoris
[ICD9: 413   ICD10: I20]
[1]
Autoimmune diseases
[ICD9: 279.4   ICD10: D84.9, M35.9]
[2]
Brain tumors
[ICD9: 191, 225.0   ICD10: C71, D33]
[3]
Breast cancer
[ICD9: 174, 175   ICD10: C50]
[4]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[2]
Colorectal cancer
[ICD9: 153, 154   ICD10: C18-C21]
[5]
Dementia
[ICD9: 290-294   ICD10: F01-F07]
[6]
Melanoma
[ICD9: 172   ICD10: C43]
[7]
Myocardial ischemia
[ICD9: 459.89   ICD10: I99.8]
[1]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[2]
Neurological diseases[8]
Photodynamic tumor
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[9]
Porphyrin-derived photocytotoxicity[10]
Viral infection, unspecified
[ICD9: 001-139, 042-075   ICD10: A00-B99, A80-A99, B00-B34]
[11]
Drug(s)AdinazolamApprovedAnxiety and status epilepticus[12]
ChlormezanoneApprovedSpasms, Pain[13]
CinolazepamApprovedMuscle Relaxant[14]
DextofisopamPhase IIIrritable bowel syndrome[15]
EmapunilDiscontinued in Phase IISevere Mood Disorders[16]
BioChemical ClassTransmembrane protein    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP30536
FunctionResponsible for the manifestation of peripheral-type benzodiazepine recognition sites and is most likely to comprise binding domains for benzodiazepines and isoquinoline carboxamides. May play a role in the transport of porphyrins and heme.    
SequenceMAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA ATTVAWYQVSPLAARLLYPYLAWLAFATTLNYCVWRDNHGWHGGRRLPE
Target ValidationClick to Find Target Validation Information.    
Inhibitor (R)PK-11195[17]
2- (2-Phenyl-1H-indol-3-yl)-N,N-dipropyl-acetamide[18]
4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene[19]
5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one[20]
5-Phenyl-6-thia-10b-aza-benzo[e]azulene[19]
6-Thia-10b-aza-benzo[e]azulen-4-one[20]
ALPIDEM[21]
N,N-Diethyl-2- (2-phenyl-1H-indol-3-yl)-acetamide[18]
N,N-Dihexyl-2- (2-phenyl-1H-indol-3-yl)-acetamide[18]
N,N-Dimethyl-2- (2-phenyl-1H-indol-3-yl)-acetamide[18]
N-Hexyl-2- (2-phenyl-1H-indol-3-yl)-acetamide[18]
PK-11195[22]
PK-11195[23]
Ro-5-4864[24]
AgonistAdinazolam[12]
Chlormezanone[13]
Dextofisopam[15]
Emapunil[16]
S-8510
SuppressorGinkgolide B (GKB)[4]
BinderCinolazepam[14]
LigandFGIN-1-27[5]
PK 11195[5]
PK11195[10][7]
Ro 5-4864[5][7]
MultitargetDextofisopam[15]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1PK 11195, an antagonist of peripheral benzodiazepine receptors, reduces ventricular arrhythmias during myocardial ischemia and reperfusion in the dog. Eur J Pharmacol. 1985 Jun 7;112(2):257-60. To Reference
Ref 2The peripheral benzodiazepine receptor: a promising therapeutic drug target. Curr Med Chem. 2003 Aug;10(16):1563-72. To Reference
Ref 3Targeted delivery of a peripheral benzodiazepine receptor ligand-gemcitabine conjugate to brain tumors in a xenograft model. Cancer Chemother Pharmacol. 2001 Aug;48(2):169-76. To Reference
Ref 4Drug-induced inhibition of the peripheral-type benzodiazepine receptor expression and cell proliferation in human breast cancer cells. Anticancer Res. 2000 Sep-Oct;20(5A):2835-47. To Reference
Ref 5Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells. Br J Cancer. 2001 Nov 30;85(11):1771-80. To Reference
Ref 6Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 7Antiproliferative and differentiating effects of benzodiazepine receptor ligands on B16 melanoma cells. Biochem Pharmacol. 1998 Oct 15;56(8):1029-34. To Reference
Ref 8Mitochondrial benzodiazepine receptors (MBR) in association with neurological disorders. Nihon Shinkei Seishin Yakurigaku Zasshi. 1998 Apr;18(2):49-54. To Reference
Ref 9Photodynamic tumor therapy: mitochondrial benzodiazepine receptors as a therapeutic target. Mol Med. 1998 Jan;4(1):40-5. To Reference
Ref 10The peripheral benzodiazepine receptor in photodynamic therapy with the phthalocyanine photosensitizer Pc 4. Photochem Photobiol. 2002 Jun;75(6):652-61. To Reference
Ref 11Mitochondrial apoptosis and the peripheral benzodiazepine receptor: a novel target for viral and pharmacological manipulation. J Exp Med. 2002 Nov 4;196(9):1121-5. To Reference
Ref 12Effects of antidepressants and benzodiazepine treatments on the dendritic structure of CA3 pyramidal neurons after chronic stress. Eur J Pharmacol. 1999 Apr 29;371(2-3):113-22. To Reference
Ref 13Successful treatment of anxiety with a single night-time dose of chlormezanone: double-blind comparison with diazepam. Curr Med Res Opin. 1982;8(1):33-8. To Reference
Ref 14Short-term sleep laboratory studies with cinolazepam in situational insomnia induced by traffic noise. Int J Clin Pharmacol Res. 1987;7(5):407-18. To Reference
Ref 15Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. To Reference
Ref 16Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 17Bioorg Med Chem Lett. 2003 Jan 20;13(2):201-4.[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). To Reference
Ref 18J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. To Reference
Ref 19J Med Chem. 1995 Nov 10;38(23):4730-8.A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors. To Reference
Ref 20J Med Chem. 1994 May 13;37(10):1427-38.Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies. To Reference
Ref 21J Med Chem. 2008 Sep 25;51(18):5798-806. Epub 2008 Aug 26.Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis. To Reference
Ref 22Bioorg Med Chem Lett. 2010 Oct 1;20(19):5799-802. Epub 2010 Aug 4.Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO). To Reference
Ref 23J Med Chem. 2008 Jan 10;51(1):17-30. Epub 2007 Dec 8.Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo. To Reference
Ref 24J Med Chem. 2010 May 27;53(10):4085-93.Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization. To Reference



 

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