Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T50269
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| Former ID |
TTDR00771
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| Target Name |
Glycine receptor alpha-1 chain
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| Gene Name |
GLRA1
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| Synonyms |
Glycine receptor 48 kDa subunit; Strychnine binding subunit; Strychnine-insensitive glycine receptor; GLRA1
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| Target Type |
Successful
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| Disease | Muscle spasm [ICD10: M62.838] | ||||
| Function |
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
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| BioChemical Class |
Neurotransmitter receptor
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| Target Validation |
T50269
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| UniProt ID | |||||
| Sequence |
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ |
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| Drugs and Mode of Action | |||||
| Drug(s) | THIOCOLCHICOSIDE | Drug Info | Approved | Muscle spasm | [1] |
| D-Serine | Drug Info | Phase 4 | Discovery agent | [2], [3] | |
| Inhibitor | 10-methoxy-ginkgolide C | Drug Info | [4] | ||
| 3,14-DIDEHYDROGINKGOLIDE A | Drug Info | [4] | |||
| 3-demethoxy-3-D-lyxopyranosylaminothiocolchicine | Drug Info | [5] | |||
| 3-demethoxy-3-D-mannopyranosylaminothiocolchicine | Drug Info | [5] | |||
| 3-demethoxy-3-D-xylopyranosylaminothiocolchicine | Drug Info | [5] | |||
| 3-demethoxy-3-L-fucopyranosylaminothiocolchicine | Drug Info | [5] | |||
| 3-demethoxy-3D-glucopyranosylaminothiocolchicine | Drug Info | [5] | |||
| D-Serine | Drug Info | [6] | |||
| GINKGOLIDE A | Drug Info | [4] | |||
| Ginkgolide C | Drug Info | [4] | |||
| Ginkgolide J | Drug Info | [4] | |||
| Ginkgolide M | Drug Info | [4] | |||
| GINKOLIDE B | Drug Info | [4] | |||
| STRYCHNINE | Drug Info | [5] | |||
| THIOCOLCHICOSIDE | Drug Info | [5] | |||
| Pathways | |||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Reactome | Ligand-gated ion channel transport | ||||
| References | |||||
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 2 | (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. (Ligand id: 4171). | ||||
| REF 3 | ClinicalTrials.gov (NCT00215904) D-serine Adjuvant Treatment for Parkinson's Disease. U.S. National Institutes of Health. | ||||
| REF 4 | J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists. | ||||
| REF 5 | J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. | ||||
| REF 6 | Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. | ||||
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