Target Information

Target General Infomation
Target ID
T50269
Former ID
TTDR00771
Target Name
Glycine receptor alpha-1 chain
Gene Name
GLRA1
Synonyms
Glycine receptor 48 kDa subunit; Strychnine binding subunit; Strychnine-insensitive glycine receptor; GLRA1
Target Type
Successful
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).
BioChemical Class
Neurotransmitter receptor
Target Validation
T50269
UniProt ID
P23415
Sequence
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
Drugs and Mode of Action
Drug(s) THIOCOLCHICOSIDE Drug Info Approved Muscle spasm [551871]
D-Serine Drug Info Phase 4 Discovery agent [467510], [521721]
Inhibitor 10-methoxy-ginkgolide C Drug Info [528727]
3,14-DIDEHYDROGINKGOLIDE A Drug Info [528727]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info [528408]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info [528408]
D-Serine Drug Info [551378]
GINKGOLIDE A Drug Info [528727]
Ginkgolide C Drug Info [528727]
Ginkgolide J Drug Info [528727]
Ginkgolide M Drug Info [528727]
GINKOLIDE B Drug Info [528727]
STRYCHNINE Drug Info [528408]
THIOCOLCHICOSIDE Drug Info [528408]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Ligand-gated ion channel transport
References
Ref 467510(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 521721ClinicalTrials.gov (NCT00215904) D-serine Adjuvant Treatment for Parkinson's Disease. U.S. National Institutes of Health.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 551378Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.

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