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

Cysteinyl leukotriene receptors 1 and 2 (CysLT1R and CysLT2R) are G protein-coupled receptors that mediate the biological effects of cysteinyl leukotrienes (LTC4, LTD4, and LTE4), which are potent lipid mediators derived from arachidonic acid (UniProt: Q9Y271, Q9NS75). CysLT1R is primarily expressed in the lungs and immune cells, where its activation leads to potent bronchoconstriction, mucus secretion, and airway edema, making it a central player in the pathophysiology of asthma and allergic rhinitis (PubMed: 11133445). CysLT2R is more widely distributed, including in the heart, brain, and blood vessels, and is associated with vascular permeability and tissue fibrosis (PubMed: 11133446). While most clinically available leukotriene receptor antagonists, such as montelukast, are selective for CysLT1R, dual antagonism of both receptors is being explored for broader anti-inflammatory and cardiovascular applications (StatPearls: NBK459350). These receptors are critical therapeutic targets for managing chronic respiratory conditions and are increasingly studied for their roles in neuroinflammation and oncology. Activation of these receptors by their ligands triggers intracellular calcium mobilization and signaling pathways that amplify the inflammatory response. Therapeutic intervention typically involves small molecule antagonists that compete with leukotrienes for receptor binding sites. Safety profiles for drugs targeting these receptors are generally favorable, though they are associated with specific neuropsychiatric risks that require clinical monitoring (FDA: 2020).

Other names

CYSLTR1CYSLTR2Cysteinyl leukotriene receptor type 1Cysteinyl leukotriene receptor type 2LTD4 receptorLTC4 receptorHGNC:2582HGNC:2583

Antagonism of cysteinyl leukotriene receptors, preventing the binding of proinflammatory leukotrienes (LTC4, LTD4, and LTE4) to their respective receptors to inhibit bronchoconstriction, mucus production, and inflammatory cell recruitment (StatPearls: NBK459350).