Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T50269
(Former ID: TTDR00771)
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| Target Name |
Strychnine-binding glycine receptor (GLRA1)
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| Synonyms |
Strychnine-insensitive glycine receptor; Strychnine binding subunit; Glycine receptor 48 kDa subunit; GLRA1
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| Gene Name |
GLRA1
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| 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).
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| BioChemical Class |
Neurotransmitter receptor
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| UniProt ID | |||||
| Sequence |
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ |
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| 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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