Cysteinyl leukotriene receptor type 2 (CYSLTR2)

Cysteinyl leukotriene receptor type 2 is a G protein-coupled cell surface receptor encoded by the CYSLTR2 gene. It binds cysteinyl leukotrienes—specifically LTC₄ and LTD₄ with high affinity—to mediate various allergic, hypersensitivity, inflammatory, fibrotic, cardiovascular, and oncological processes. The gene is located on chromosome 13q14—a region linked to asthma—and encodes a seven-transmembrane domain protein expressed predominantly in heart tissue but also found in adrenals, placenta, spleen, peripheral blood leukocytes, airway smooth muscle cells, endothelial cells of certain vascular beds as well as some brain regions[1][5][7]. Activation of this receptor leads primarily to coupling with Gq proteins that trigger intracellular signaling cascades resulting in smooth muscle contraction; increased vascular permeability; recruitment of eosinophils; cytokine production; cell proliferation; plasma exudation; mucous production; cardiodepression; fibrosis development; airway remodeling during chronic inflammation; among others[1][5]. While most current anti-leukotriene drugs target its close homolog CysLT1R rather than CysLT2R due to differences in ligand sensitivity profiles and tissue distribution patterns,[6] recent structural studies have provided insights into ligand binding pockets unique to human CYSLTR2 that may facilitate rational design of new therapeutic agents for conditions where it plays a pathogenic role—including refractory asthma subtypes unresponsive to existing treatments or certain cancers where it is implicated as an emerging therapeutic target[4].

Other names

CysLT2 receptorCysLTR2Leukotriene D4 receptor 2 (less common)LTC4/LTD4 receptor type 2 (functional description)

For potential drugs targeting this molecule in the future, mechanisms would likely include antagonism or inverse agonism at the G protein-coupled receptor to inhibit downstream inflammatory signaling pathways activated by cysteinyl leukotrienes such as LTC4 and LTD4[1][5].