CysLT1R

CysLT1R, also known as the cysteinyl leukotriene receptor 1, is a G protein-coupled receptor that plays a crucial role in mediating the effects of cysteinyl leukotrienes. These potent inflammatory mediators are produced by various cells, including mast cells and eosinophils, and are involved in allergic and inflammatory responses. CysLT1R is primarily expressed on smooth muscle cells, eosinophils, and mast cells within the airways. Its activation leads to a cascade of events, including bronchoconstriction, mucus secretion, and eosinophil recruitment, which are characteristic features of conditions like asthma and allergic rhinitis. The binding of cysteinyl leukotrienes, such as leukotriene C4 (LTC4), LTD4, and LTE4, to CysLT1R triggers a conformational change in the receptor, leading to the activation of intracellular signaling pathways. These pathways involve the G protein q (Gq) and downstream effectors like phospholipase C, ultimately increasing intracellular calcium levels and leading to smooth muscle contraction. Antagonists targeting CysLT1R, known as leukotriene receptor antagonists (LTRAs), are a class of drugs used in the management of asthma and allergic rhinitis, demonstrating the therapeutic significance of this receptor. Understanding the structure, function, and signaling of CysLT1R is vital for developing more effective treatments for inflammatory airway diseases.