Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00039

Target Information
NameGlycine receptor    
Type of targetDiscontinued target    
SynonymsGLR    
Glycine receptor 58 kDa subunit    
DiseaseTobacco Dependence
[ICD9: 305.1   ICD10: F17]
[1]
Drug(s)GW 468816Suspended in Phase II in GSK 2009 ReportTobacco Dependence[2]
GW468816Suspended in Phase II in GSK 2009 ReportSmoking cessation[3]
PathwayNeuroactive ligand-receptor interaction
UniProt IDP48167
SequenceMKFLLTTAFLILISLWVEEAYSKEKSSKKGKGKKKQYLCPSQQSAEDLARVPANSTSNIL NRLLVSYDPRIRPNFKGIPVDVVVNIFINSFGSIQETTMDYRVNIFLRQKWNDPRLKLPS DFRGSDALTVDPTMYKCLWKPDLFFANEKSANFHDVTQENILLFIFRDGDVLVSMRLSIT LSCPLDLTLFPMDTQRCKMQLESFGYTTDDLRFIWQSGDPVQLEKIALPQFDIKKEDIEY GNCTKYYKGTGYYTCVEVIFTLRRQVGFYMMGVYAPTLLIVVLSWLSFWINPDASAARVP LGIFSVLSLASECTTLAAELPKVSYVKALDVWLIACLLFGFASLVEYAVVQVMLNNPKRV EAEKARIAKAEQADGKGGNVAKKNTVNGTGTPVHISTLQVGETRCKKVCTSKSDLRSNDF SIVGSLPRDFELSNYDCYGKPIEVNNGLGKSQAKNNKKPPPAKPVIPTAAKRIDLYARAL FPFCFLFFNVIYWSIYL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (12E,20Z,18S)-8-hydroxyvariabilin[4]
10-methoxy-ginkgolide C[5]
3,14-DIDEHYDROGINKGOLIDE A[5]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine[6]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine[6]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine[6]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine[6]
3-demethoxy-3D-glucopyranosylaminothiocolchicine[6]
GINKGOLIDE A[5]
GINKOLIDE B[5]
ORG-25543[7]
PICROTIN[8]
STRYCHNINE[6]
THIOCOLCHICOSIDE[6]
ginkgolide C[5]
ginkgolide J[5]
ginkgolide M[5]
AntagonistGW 468816[2]
GW468816[3]
Gavestinel[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 2Executive summary: nicotine addiction. Drugs Today (Barc). 2005 Jun;41(6):419-25. To Reference
Ref 3GSK. Product Development Pipeline. February 2009. To Reference
Ref 4Bioorg 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. To Reference
Ref 5J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists. To Reference
Ref 6J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. To Reference
Ref 7J Med Chem. 2001 Aug 16;44(17):2679-82.The first potent and selective inhibitors of the glycine transporter type 2. To Reference
Ref 8J Biol Chem. 2007 Jun 1;282(22):16016-35. Epub 2007 Apr 3.Mechanisms for picrotoxinin and picrotin blocks of alpha2 homomeric glycine receptors. To Reference
Ref 9Neuroprotective agents for the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2003 Jan;3(1):9-20. To Reference



 

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