Target General Infomation
Target ID
T50269 (Former ID: TTDR00771)
Target Name
Strychnine-binding glycine receptor (GLRA1)
Synonyms
Strychnine-insensitive glycine receptor; Strychnine binding subunit; Glycine receptor 48 kDa subunit; GLRA1
Gene Name
GLRA1
Target Type
Successful target
[1]
Disease [+] 1 Target-related Diseases +
1 Tonus and reflex abnormality [ICD-11: MB47]
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
UniProt ID
GLRA1_HUMAN
Sequence
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 THIOCOLCHICOSIDE Drug Info Approved Muscle spasm [2]
Mode of Action [+] 1 Modes of Action +
Inhibitor [+] 15 Inhibitor drugs +
1 THIOCOLCHICOSIDE Drug Info [1]
2 D-Serine Drug Info [3]
3 10-methoxy-ginkgolide C Drug Info [4]
4 3,14-DIDEHYDROGINKGOLIDE A Drug Info [4]
5 3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info [1]
6 3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info [1]
7 3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info [1]
8 3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info [1]
9 3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info [1]
10 GINKGOLIDE A Drug Info [4]
11 Ginkgolide C Drug Info [4]
12 Ginkgolide J Drug Info [4]
13 Ginkgolide M Drug Info [4]
14 GINKOLIDE B Drug Info [4]
15 [3H]strychnine Drug Info [1]
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Neuroactive ligand-receptor interaction
Reactome [+] 1 Reactome Pathways +
1 Ligand-gated ion channel transport
Target-Related Models and Studies
Target Validation
References
REF 1 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
REF 2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3 Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
REF 4 Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7.

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