Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T73724
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| Former ID |
TTDR00164
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| Target Name |
Neuronal acetylcholine receptor protein, beta-4 chain
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| Gene Name |
CHRNB4
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| Synonyms |
Beta-4 nAChR; CHRNB4
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| Target Type |
Discontinued
|
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| Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
| Function |
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
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| BioChemical Class |
Ion transport
|
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| Target Validation |
T73724
|
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| UniProt ID | |||||
| Sequence |
MRRAPSLVLFFLVALCGRGNCRVANAEEKLMDDLLNKTRYNNLIRPATSSSQLISIKLQL
SLAQLISVNEREQIMTTNVWLKQEWTDYRLTWNSSRYEGVNILRIPAKRIWLPDIVLYNN ADGTYEVSVYTNLIVRSNGSVLWLPPAIYKSACKIEVKYFPFDQQNCTLKFRSWTYDHTE IDMVLMTPTASMDDFTPSGEWDIVALPGRRTVNPQDPSYVDVTYDFIIKRKPLFYTINLI IPCVLTTLLAILVFYLPSDCGEKMTLCISVLLALTFFLLLISKIVPPTSLDVPLIGKYLM FTMVLVTFSIVTSVCVLNVHHRSPSTHTMAPWVKRCFLHKLPTFLFMKRPGPDSSPARAF PPSKSCVTKPEATATSTSPSNFYGNSMYFVNPASAASKSPAGSTPVAIPRDFWLRSSGRF RQDVQEALEGVSFIAQHMKNDDEDQSVVEDWKYVAMVVDRLFLWVFMFVCVLGTVGLFLP PLFQTHAASEGPYAAQRD |
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| Drugs and Mode of Action | |||||
| Drug(s) | SIB-1553A | Drug Info | Discontinued in Phase 2 | Alzheimer disease | [1] |
| HOMOEPIBATIDINE | Drug Info | Terminated | Discovery agent | [2] | |
| Inhibitor | (2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol | Drug Info | [3] | ||
| (2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol | Drug Info | [3] | |||
| 15-nor-18-Methoxycornaridine | Drug Info | [4] | |||
| 18-Dimethylaminocoronaridine | Drug Info | [4] | |||
| 18-methoxycoronaridinate 2-Hydroxyethylamide | Drug Info | [4] | |||
| 18-methoxycoronaridinate 2-methoxyethylamide | Drug Info | [4] | |||
| 18-Methylaminocoronaridine | Drug Info | [4] | |||
| 2-Acetylaminoethyl 18-methoxycoronaridinate | Drug Info | [4] | |||
| 2-Hydroxyethyl 18-methoxycoronaridinate | Drug Info | [4] | |||
| 2-Methoxyethyl 18-methoxycoronaridinate | Drug Info | [4] | |||
| CYTISINE | Drug Info | [5] | |||
| GCCSNPVCHLEHSNLC* | Drug Info | [6] | |||
| HOMOEPIBATIDINE | Drug Info | [7] | |||
| N,N-Dimethylaminoethyl 18-methoxycoronaridinate | Drug Info | [4] | |||
| Agonist | SIB-1553A | Drug Info | [8] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Cholinergic synapse | |||||
| PANTHER Pathway | Nicotinic acetylcholine receptor signaling pathway | ||||
| Nicotine pharmacodynamics pathway | |||||
| Reactome | Highly sodium permeable acetylcholine nicotinic receptors | ||||
| Highly calcium permeable postsynaptic nicotinic acetylcholine receptors | |||||
| Highly calcium permeable nicotinic acetylcholine receptors | |||||
| WikiPathways | SIDS Susceptibility Pathways | ||||
| Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | |||||
| Nicotine Activity on Chromaffin Cells | |||||
| References | |||||
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009631) | ||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007531) | ||||
| REF 3 | J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. | ||||
| REF 4 | J Med Chem. 2003 Jun 19;46(13):2716-30.Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents. | ||||
| REF 5 | Bioorg Med Chem Lett. 2008 Apr 1;18(7):2316-9. Epub 2008 Mar 6.Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine. | ||||
| REF 6 | J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. | ||||
| REF 7 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships. | ||||
| REF 8 | SIB-1553A, (+/-)-4-[[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride, a subtype-selective ligand for nicotinic acetylcholine receptors with putative cognitive-enhancing properties: effectson working and reference memory performances in aged rodents and nonhuman primates. J Pharmacol Exp Ther. 2001 Oct;299(1):297-306. | ||||
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