Target Information
Target General Infomation | |||||
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Target ID |
T26368
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Former ID |
TTDR01042
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Target Name |
Gamma-aminobutyric-acid receptor alpha-5 subunit
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Gene Name |
GABRA5
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Synonyms |
GABA-A alpha-5; GABAA alpha 5; GABRA5
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Target Type |
Clinical Trial
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3] | |||||
Function |
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
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BioChemical Class |
Ligand-gated ion channel
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Target Validation |
T26368
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UniProt ID | |||||
Sequence |
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK |
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Drugs and Mode of Action | |||||
Inhibitor | (2E,4S)-4-ammoniopent-2-enoate | Drug Info | [533514] | ||
(4R)-4-ammoniopentanoate | Drug Info | [533514] | |||
(4S)-4-ammoniopentanoate | Drug Info | [533514] | |||
3-(benzyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-(isopentyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-butoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-ethoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-isobutoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-propoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
5-[(1R)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [533514] | |||
5-[(1S)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [533514] | |||
AMENTOFLAVONE | Drug Info | [526653] | |||
Barbituric acid derivative | Drug Info | [551407] | |||
Beta-Carboline-3-carboxylic acid t-butyl ester | Drug Info | [531188] | |||
CI-218872 | Drug Info | [531188] | |||
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
GAMMA-AMINO-BUTANOIC ACID | Drug Info | [533580] | |||
L-655708 | Drug Info | [527005] | |||
Ro-151310 | Drug Info | [531044] | |||
Ro-154513 | Drug Info | [534122] | |||
Ro-4938581 | Drug Info | [530391] | |||
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
Modulator (allosteric modulator) | alpha3IA | Drug Info | [543811] | ||
alpha5IA | Drug Info | [543811] | |||
DMCM | Drug Info | [543811] | |||
RY024 | Drug Info | [543811] | |||
tetrahydrodeoxycorticosterone | Drug Info | [543811] | |||
TP003 | Drug Info | [543811] | |||
[11C]flumazenil | Drug Info | [543811] | |||
[18F]fluoroethylflumazenil | Drug Info | [543811] | |||
[3H]CGS8216 | Drug Info | [543811] | |||
[3H]L655708 | Drug Info | [543811] | |||
Agonist | HT-2678 | Drug Info | [543811] | ||
isonipecotic acid | Drug Info | [543811] | |||
piperidine-4-sulphonic acid | Drug Info | [543811] | |||
RG-1662 | Drug Info | [551418] | |||
[3H]muscimol | Drug Info | [543811] | |||
Blocker (channel blocker) | TBPS | Drug Info | [543811] | ||
[35S]TBPS | Drug Info | [543811] | |||
Modulator | [3H]RY80 | Drug Info | [534498] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Retrograde endocannabinoid signaling | |||||
GABAergic synapse | |||||
Morphine addiction | |||||
Nicotine addiction | |||||
Reactome | Ligand-gated ion channel transport | ||||
GABA A receptor activation | |||||
WikiPathways | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | ||||
Iron uptake and transport | |||||
References | |||||
Ref 526653 | Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. | ||||
Ref 527005 | J 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. | ||||
Ref 530391 | Bioorg 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. | ||||
Ref 531044 | Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. | ||||
Ref 531188 | Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. | ||||
Ref 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 533580 | J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. | ||||
Ref 534122 | J 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. | ||||
Ref 534498 | [3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits. J Pharmacol Exp Ther. 1997 Nov;283(2):488-93. | ||||
Ref 543811 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 408). |
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