Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01042

Target Information
NameGamma-aminobutyric-acid receptor alpha-5 subunit    
Type of targetClinical trial target    
SynonymsGABA-A alpha-5    
GABAA alpha 5    
DiseaseAlzheimer's Disease
[ICD9: 331.0   ICD10: G30]
[1]
Central nervous system diseases
[ICD9: 294.1, 307.23, 314.00, 314.01, 320-322, 323, 331.0, 332, 333.4, 340, 344.1, 344.81, 348.0   ICD10: A83-A86, B94.1, F02.2, F02.3, F90, F95.2, G00-G37, G83.5, G93.0]
[1]
Cognitive deficits
[ICD9: 290-294, 294.0, 780.09, 780.9, 780.93   ICD10: F01-F07, F04, R41.3]
[1]
Delirium
[ICD9: 293   ICD10: F05]
[1]
Dementia
[ICD9: 290-294   ICD10: F01-F07]
[1]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP31644
FunctionGaba, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the gaba/benzodiazepine receptor and opening an integral chloride channel.    
SequenceMDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
Related US Patent6,455,552
6,534,505
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2E,4S)-4-ammoniopent-2-enoate[2]
(4R)-4-ammoniopentanoate[2]
(4S)-4-ammoniopentanoate[2]
3- (benzyloxy)-9H-pyrido[3,4-b]indole[3]
3- (hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole[3]
3- (isopentyloxy)-9H-pyrido[3,4-b]indole[3]
3-butoxy-9H-pyrido[3,4-b]indole[3]
3-ethoxy-9H-pyrido[3,4-b]indole[3]
3-isobutoxy-9H-pyrido[3,4-b]indole[3]
3-propoxy-9H-pyrido[3,4-b]indole[3]
5-[ (1R)-1-ammonioethyl]isoxazol-3-olate[2]
5-[ (1S)-1-ammonioethyl]isoxazol-3-olate[2]
AMENTOFLAVONE[4]
Barbital[5]
Barbituric acid derivative[5]
CI-218872[3]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate[3]
GAMMA-AMINO-BUTANOIC ACID[6]
L-655708,   NCGC00025115-02[7]
Ro-151310[8]
Ro-154513[9]
Ro-4882224[10]
Ro-4938581[10]
TPA-023[11]
beta-Carboline-3-carboxylic acid t-butyl ester[3]
ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate[3]
sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 2J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 3Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. To Reference
Ref 4Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 5Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. To Reference
Ref 6J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. To Reference
Ref 7J Med Chem. 2004 Mar 25;47(7):1807-22.3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. To Reference
Ref 8Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. To Reference
Ref 9J Med Chem. 1996 Apr 26;39(9):1928-34.Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors. To Reference
Ref 10Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction. To Reference
Ref 11J Med Chem. 2006 Jan 12;49(1):35-8.Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. To Reference



 

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