Cysteinyl leukotriene receptor 1 and Cysteinyl leukotriene receptor 2 (CysLT1 receptor (CysLT1R) and CysLT2 receptor (CysLT2R))

Cysteinyl leukotriene receptors 1 and 2 (CysLT1R and CysLT2R) are G protein-coupled receptors responsible for mediating the effects of cysteinyl leukotrienes (LTC4, LTD4, LTE4), which are lipid mediators produced via the 5-lipoxygenase pathway. These receptors play central roles in the pathogenesis of inflammatory disorders such as asthma, allergic rhinitis, atherosclerosis, and have emerging significance in cancer and central nervous system pathology[1][2][4]. CysLT1R is most responsive to LTD4 and is primarily expressed in spleen, leukocytes, and airway smooth muscle[4]. CysLT2R responds equally to LTC4 and LTD4 and is expressed in heart, adrenal, placenta, and certain immune and brain cells[4]. Both receptors mediate bronchoconstriction, leukocyte trafficking, and increased vascular permeability. Selective CysLT1 antagonists (montelukast, zafirlukast, pranlukast) are widely used for asthma and allergy management, but receptor subtype-specific inhibitors for CysLT2 are not yet clinically available. Recent advances in structural biology have revealed unique ligand binding and activation mechanisms for both receptors, guiding efforts to develop safer and more effective therapies for inflammation and malignancy[1][2].

Other names

CysLT1CysLT1RCysteinyl leukotriene receptor type 1CysLT2CysLT2RCysteinyl leukotriene receptor type 2

Antagonism of CysLT1 receptor to block cysteinyl leukotriene-induced inflammatory responses. This prevents bronchoconstriction, reduces eosinophilic inflammation, and limits vascular permeability. - CysLT2 receptor antagonists are under investigation but not broadly available.