Target Information
Target General Infomation | |||||
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Target ID |
T55285
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Former ID |
TTDC00039
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Target Name |
Glycine receptor
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Gene Name |
GLRB
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Synonyms |
GLR; Glycine receptor 58 kDa subunit; GLRB
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Target Type |
Successful
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Disease | Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | ||||
Epilepsy [ICD10: G40] | |||||
Muscle spasm [ICD10: M62.838] | |||||
Migraine [ICD9: 346; ICD10: G43] | |||||
Nerve injury [ICD10: T14.4] | |||||
Tobacco dependence [ICD9: 305.1; ICD10: F17] | |||||
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 |
T55285
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UniProt ID | |||||
Sequence |
MKFLLTTAFLILISLWVEEAYSKEKSSKKGKGKKKQYLCPSQQSAEDLARVPANSTSNIL
NRLLVSYDPRIRPNFKGIPVDVVVNIFINSFGSIQETTMDYRVNIFLRQKWNDPRLKLPS DFRGSDALTVDPTMYKCLWKPDLFFANEKSANFHDVTQENILLFIFRDGDVLVSMRLSIT LSCPLDLTLFPMDTQRCKMQLESFGYTTDDLRFIWQSGDPVQLEKIALPQFDIKKEDIEY GNCTKYYKGTGYYTCVEVIFTLRRQVGFYMMGVYAPTLLIVVLSWLSFWINPDASAARVP LGIFSVLSLASECTTLAAELPKVSYVKALDVWLIACLLFGFASLVEYAVVQVMLNNPKRV EAEKARIAKAEQADGKGGNVAKKNTVNGTGTPVHISTLQVGETRCKKVCTSKSDLRSNDF SIVGSLPRDFELSNYDCYGKPIEVNNGLGKSQAKNNKKPPPAKPVIPTAAKRIDLYARAL FPFCFLFFNVIYWSIYL |
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Structure |
1MOT; 1VRY; 2M6B; 2M6I
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Drugs and Mode of Action | |||||
Drug(s) | THIOCOLCHICOSIDE | Drug Info | Approved | Muscle spasm | [551871] |
MDL-27531 | Drug Info | Phase 1 | Epilepsy | [526961] | |
UK-240455 | Drug Info | Phase 1 | Nerve injury | [526291] | |
ZD-9379 | Drug Info | Phase 1 | Cerebrovascular ischaemia | [526658], [534544] | |
Gavestinel | Drug Info | Discontinued in Phase 2 | Nerve injury | [546403] | |
GV-196771 | Drug Info | Discontinued in Phase 2 | Migraine | [467542], [546551] | |
GW 468816 | Drug Info | Discontinued in Phase 2 | Tobacco dependence | [536129] | |
M-241247 | Drug Info | Terminated | Cerebrovascular ischaemia | [545475] | |
Inhibitor | (12E,20Z,18S)-8-hydroxyvariabilin | Drug Info | [530814] | ||
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] | |||
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] | |||
PICROTIN | Drug Info | [528770] | |||
STRYCHNINE | Drug Info | [528408] | |||
THIOCOLCHICOSIDE | Drug Info | [528408] | |||
Antagonist | bilobalide | Drug Info | [543824] | ||
ginkgolide X | Drug Info | [543824] | |||
M-241247 | Drug Info | [545476] | |||
PMBA | Drug Info | [543823] | |||
[3H]strychnine | Drug Info | [543823] | |||
Blocker (channel blocker) | cyanotriphenylborate | Drug Info | [533882] | ||
Modulator | Gavestinel | Drug Info | |||
GV-196771 | Drug Info | [525509] | |||
GW 468816 | Drug Info | ||||
MDL-27531 | Drug Info | [526961] | |||
UK-240455 | Drug Info | [526291] | |||
ZD-9379 | Drug Info | [526658], [534544] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Reactome | Ligand-gated ion channel transport | ||||
WikiPathways | Iron uptake and transport | ||||
References | |||||
Ref 467542 | (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: 4208). | ||||
Ref 526658 | Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26. | ||||
Ref 526961 | MDL 27,531 reduces spontaneous hindlimb contractions in rats with chronic transections of the spinal cord. Neurosci Lett. 1992 Nov 23;147(1):101-5. | ||||
Ref 534544 | A glycine site antagonist, ZD9379, reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion. Stroke. 1998 Jan;29(1):190-5. | ||||
Ref 545475 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415) | ||||
Ref 546403 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007924) | ||||
Ref 525509 | First time in human for GV196771: interspecies scaling applied on dose selection. J Clin Pharmacol. 1999 Jun;39(6):560-6. | ||||
Ref 526658 | Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26. | ||||
Ref 526961 | MDL 27,531 reduces spontaneous hindlimb contractions in rats with chronic transections of the spinal cord. Neurosci Lett. 1992 Nov 23;147(1):101-5. | ||||
Ref 528408 | 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 528727 | J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists. | ||||
Ref 528770 | J Biol Chem. 2007 Jun 1;282(22):16016-35. Epub 2007 Apr 3.Mechanisms for picrotoxinin and picrotin blocks of alpha2 homomeric glycine receptors. | ||||
Ref 530814 | Bioorg Med Chem. 2010 Apr 15;18(8):2912-9. Epub 2010 Mar 6.Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. | ||||
Ref 533882 | Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels. Proc Natl Acad Sci U S A. 1994 Sep 13;91(19):8950-4. | ||||
Ref 534544 | A glycine site antagonist, ZD9379, reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion. Stroke. 1998 Jan;29(1):190-5. | ||||
Ref 543823 | (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. (Target id: 425). |
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