Cysteinyl leukotriene receptor 1 (CYSLTR1) (CYSLTR1)

The Cysteinyl leukotriene receptor 1 (CysLT1) is a G protein-coupled receptor primarily expressed in human airway smooth muscle cells, interstitial macrophages, and various inflammatory cells like eosinophils and mast cells [1, 2]. It serves as a high-affinity receptor for cysteinyl leukotrienes, particularly leukotriene D4 (LTD4), which are potent lipid mediators derived from arachidonic acid [1, 3]. Upon activation, CysLT1 triggers intracellular signaling pathways that lead to potent bronchoconstriction, increased vascular permeability, and enhanced mucus secretion, making it a central player in the pathophysiology of respiratory diseases [2, 4]. Consequently, CysLT1 is a major therapeutic target for the treatment of chronic asthma and allergic rhinitis [5]. Drugs such as montelukast and zafirlukast act as selective antagonists of this receptor, effectively blocking the pro-inflammatory and bronchoconstrictive effects of leukotrienes [5, 6]. Beyond respiratory conditions, emerging research suggests CysLT1 may play roles in cardiovascular diseases and certain types of cancer, although these remain areas of active investigation [7, 8].

Other names

CysLT1 receptorCYSLT1Cysteinyl leukotriene receptor type 1LTD4 receptorG-protein coupled receptor 106GPR106HMTMF81HGNC:2582

Competitive antagonism of the cysteinyl leukotriene receptor 1, which prevents the binding of cysteinyl leukotrienes such as LTD4, thereby inhibiting bronchoconstriction, airway edema, and inflammatory cell recruitment.