Target Information

Target General Infomation
Target ID
T74238
Former ID
TTDI01916
Target Name
Leukotriene CysLT2 receptor
Gene Name
CYSLTR2
Synonyms
CysLTR2; Cysteinyl leukotriene receptor 2; Gprotein coupled receptor GPCR21; Gprotein coupled receptor HG57; HPN321; hGPCR21; CYSLTR2
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Unspecified [ICD code not available]
Function
Receptor for cysteinyl leukotrienes. The response is mediated via a G-protein that activates a phosphatidylinositol- calcium second messenger system. Stimulation by BAY u9773, a partial agonist, induces specific contractions of pulmonary veinsand might also have an indirect role in the relaxation of the pulmonary vascular endothelium. The rank order of affinities for the leukotrienes is LTC4 = LTD4 >> LTE4.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q9NS75
Sequence
MERKFMSLQPSISVSEMEPNGTFSNNNSRNCTIENFKREFFPIVYLIIFFWGVLGNGLSI
YVFLQPYKKSTSVNVFMLNLAISDLLFISTLPFRADYYLRGSNWIFGDLACRIMSYSLYV
NMYSSIYFLTVLSVVRFLAMVHPFRLLHVTSIRSAWILCGIIWILIMASSIMLLDSGSEQ
NGSVTSCLELNLYKIAKLQTMNYIALVVGCLLPFFTLSICYLLIIRVLLKVEVPESGLRV
SHRKALTTIIITLIIFFLCFLPYHTLRTVHLTTWKVGLCKDRLHKALVITLALAAANACF
NPLLYYFAGENFKDRLKSALRKGHPQKAKTKCVFPVSVWLRKETRV
Drugs and Mode of Action
Drug(s) BAY-X-7195 Drug Info Phase 2 Asthma [1]
AS-35 Drug Info Discontinued in Phase 2 Asthma [2]
DS-4574 Drug Info Discontinued in Phase 2 Asthma [3]
Sulukast Drug Info Discontinued in Phase 2 Asthma [4], [5]
FPL-55712 Drug Info Terminated Asthma [6]
LY-290154 Drug Info Terminated Asthma [7]
MDL-43291 Drug Info Terminated Asthma [8]
Modulator AS-35 Drug Info [9]
BAY-X-7195 Drug Info
CGP-57698 Drug Info
DS-4574 Drug Info [10]
FPL-55712 Drug Info [11]
LY-290154 Drug Info
MDL-43291 Drug Info
Sulukast Drug Info
Antagonist BayCysLT2 Drug Info [12]
BAYu9773 Drug Info [13]
HAMI3379 Drug Info [14]
pobilukast Drug Info [15]
[3H]ICI-198615 Drug Info [16]
Agonist LTC4 Drug Info [17]
LTD4 Drug Info [17]
LTE4 Drug Info [18]
N-methyl LTC4 Drug Info [18]
[3H]LTC4 Drug Info [19]
[3H]LTD4 Drug Info [20]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
NetPath Pathway IL4 Signaling Pathway
IL3 Signaling Pathway
Pathway Interaction Database Endothelins
Reactome Leukotriene receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003794)
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001439)
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000587)
REF 4(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: 3327).
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000090)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000089)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007201)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000087)
REF 9Peptide leukotriene antagonistic activity of AS-35, a new antiallergic drug. Jpn J Pharmacol. 1992 Apr;58(4):347-55.
REF 10Inhibitory effect of DS-4574, a mast cell stabilizer with peptidoleukotriene receptor antagonism, on gastric acid secretion in rats. Eur J Pharmacol. 1994 Apr 1;255(1-3):229-34.
REF 11Effect of the leukotriene receptor antagonists FPL 55712, LY 163443, and MK-571 on the elimination of cysteinyl leukotrienes in the rat. Br J Pharmacol. 1991 Apr;102(4):865-70.
REF 12Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor. FASEB J. 2011 Oct;25(10):3519-28.
REF 13BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur J Pharmacol. 1994 Nov 3;264(3):317-23.
REF 14Pharmacological characterization of the first potent and selective antagonist at the cysteinyl leukotriene 2 (CysLT(2)) receptor. Br J Pharmacol. 2010 May;160(2):399-409.
REF 15(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: 270).
REF 16Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
REF 17Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.
REF 18Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT?? agonist, N-methyl-leukotriene C?? in calcium reporter and beta arrestin assays. Mol Pharmacol. 2011 Feb;79(2):270-8.
REF 19The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor. Biochem Biophys Res Commun. 2000 Aug 2;274(2):316-22.
REF 20Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem. 2000 Sep 29;275(39):30531-6.

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