Target Information

Target General Infomation
Target ID
T55285
Former ID
TTDC00039
Target Name
Glycine receptor
Gene Name
GLRB
Synonyms
GLR; Glycine receptor 58 kDa subunit; GLRB
Target Type
Successful
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).
BioChemical Class
Neurotransmitter receptor
Target Validation
T55285
UniProt ID
P48167
Sequence
MKFLLTTAFLILISLWVEEAYSKEKSSKKGKGKKKQYLCPSQQSAEDLARVPANSTSNIL
NRLLVSYDPRIRPNFKGIPVDVVVNIFINSFGSIQETTMDYRVNIFLRQKWNDPRLKLPS
DFRGSDALTVDPTMYKCLWKPDLFFANEKSANFHDVTQENILLFIFRDGDVLVSMRLSIT
LSCPLDLTLFPMDTQRCKMQLESFGYTTDDLRFIWQSGDPVQLEKIALPQFDIKKEDIEY
GNCTKYYKGTGYYTCVEVIFTLRRQVGFYMMGVYAPTLLIVVLSWLSFWINPDASAARVP
LGIFSVLSLASECTTLAAELPKVSYVKALDVWLIACLLFGFASLVEYAVVQVMLNNPKRV
EAEKARIAKAEQADGKGGNVAKKNTVNGTGTPVHISTLQVGETRCKKVCTSKSDLRSNDF
SIVGSLPRDFELSNYDCYGKPIEVNNGLGKSQAKNNKKPPPAKPVIPTAAKRIDLYARAL
FPFCFLFFNVIYWSIYL
Structure
1MOT; 1VRY; 2M6B; 2M6I
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 526291UK-315716/UK-240455. Pfizer. Curr Opin Investig Drugs. 2001 Dec;2(12):1737-9.
Ref 526658Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26.
Ref 526961MDL 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 534544A 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 536129Executive summary: nicotine addiction. Drugs Today (Barc). 2005 Jun;41(6):419-25.
Ref 545475Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)
Ref 546403Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007924)
Ref 546551Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008901)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525509First time in human for GV196771: interspecies scaling applied on dose selection. J Clin Pharmacol. 1999 Jun;39(6):560-6.
Ref 526291UK-315716/UK-240455. Pfizer. Curr Opin Investig Drugs. 2001 Dec;2(12):1737-9.
Ref 526658Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotox Res. 2002 Mar;4(2):119-26.
Ref 526961MDL 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 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 528770J 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 530814Bioorg 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 533882Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels. Proc Natl Acad Sci U S A. 1994 Sep 13;91(19):8950-4.
Ref 534544A 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).
Ref 543824(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: 427).
Ref 545476Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003415)

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