Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TT0PZR5)

• DTT Name: Leukotriene CysLT2 receptor (CYSLTR2) DTT Info
• Gene Name: CYSLTR2

Molecule-Related Drug & Molecule List

1 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[1]

7 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AS-35	DMC2WI7	Asthma	CA23	Discontinued in Phase 2	[2]
DS-4574	DM8GZWC	Asthma	CA23	Discontinued in Phase 2	[3]
Sulukast	DMBSLZV	Asthma	CA23	Discontinued in Phase 2	[4]
FPL-55712	DMF1CDK	Asthma	CA23	Terminated	[5]
ICI-198615	DM0195G	Asthma	CA23	Terminated	[6]
LY-290154	DMPZ7AO	Asthma	CA23	Terminated	[7]
MDL-43291	DMBIDQX	Asthma	CA23	Terminated	[8]

10 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BayCysLT2	DMKFTZA	Discovery agent	N.A.	Investigative	[9]
BAYu9773	DMXQ14V	Discovery agent	N.A.	Investigative	[10]
CGP-57698	DMYZ72J	Discovery agent	N.A.	Investigative	[11]
HAMI3379	DMJN0BL	Discovery agent	N.A.	Investigative	[12]
LTC4	DM702WR	Discovery agent	N.A.	Investigative	[13]
LTD4	DMIUZX3	Discovery agent	N.A.	Investigative	[13]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[14]
N-methyl LTC4	DM6XYCU	Discovery agent	N.A.	Investigative	[14]
pobilukast	DMURB4Y	Discovery agent	N.A.	Investigative	[15]
[3H]LTC4	DMD09BO	Discovery agent	N.A.	Investigative	[16]

References

• [1] The effect of a novel leukotriene C4/D4 antagonist, BAY-x-7195, on experimental allergic reactions. Prostaglandins. 1995 Nov-Dec;50(5-6):269-85.
• [2] Inhibition of radiolabeled leukotriene-binding by AS-35 in guinea pig lung membrane fraction. Jpn J Pharmacol. 1992 Apr;58(4):357-64.
• [3] Inhibitory 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.
• [4] The pharmacological evaluation of LY 170680, a novel leukotriene D4 and E4 antagonist in the guinea-pig. Br J Pharmacol. 1989 Sep;98(1):259-67.
• [5] Effect 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.
• [6] Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
• [7] DOI: 10.1021/op060036x
• [8] Conformationally restricted leukotriene receptor antagonists: [(octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]ace tic acids. Pharmacology. 1990;40(5):271-6.
• [9] Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor. FASEB J. 2011 Oct;25(10):3519-28.
• [10] BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur J Pharmacol. 1994 Nov 3;264(3):317-23.
• [11] A kinetic binding study to evaluate the pharmacological profile of a specific leukotriene C(4) binding site not coupled to contraction in human lun... Mol Pharmacol. 2000 Jun;57(6):1182-9.
• [12] Pharmacological 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.
• [13] Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.
• [14] Differential 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.
• [15] URL: 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).
• [16] The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT(2) receptor. Biochem Biophys Res Commun. 2000 Aug 2;274(2):316-22.