Target intelligence / Profile preview

Cysteinyl-leukotriene Receptor (CysLTR)

Target
CysLTR
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The cysteinyl-leukotriene receptors (CysLTRs) are G protein–coupled receptors (GPCRs) that mediate the biological effects of cysteinyl leukotrienes (CysLTs), which are lipid mediators derived from arachidonic acid metabolism. There are two main subtypes: CysLT1R and CysLT2R, both of which play significant roles in inflammatory processes. Activation of these receptors leads to airway bronchoconstriction, increased vascular permeability and edema, recruitment of eosinophils and neutrophils, smooth muscle proliferation and fibrosis, and mucin secretion, contributing to the pathogenesis of asthma, allergic rhinitis, cardiovascular diseases, and potentially other conditions like certain cancers and CNS disorders.

Other names
Cysteinyl Leukotriene ReceptorCysLT ReceptorLeukotriene Receptor
02

Mechanism of action

CysLT1 receptor antagonism

03

Biological functions

Signal transductionBronchoconstrictionInflammationVascular permeabilityImmune responseSmooth muscle proliferationMucin secretion
04

Disease associations

AsthmaAllergic rhinitisCardiovascular diseaseCancerBrain injuryMultiple sclerosisAlzheimer’s diseaseParkinson’s disease
05

Safety considerations

Variable efficacy among patientsSide effects associated with CysLT1 receptor antagonists
06

Interacting drugs

Montelukast

2 more in the full profile.

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