Cysteinyl leukotriene receptor family is a G protein-coupled receptor family that binds cysteinyl leukotrienes which are produced predominantly by myeloid cells associated with various inflammatory responses. Studies have shown that cysteinyl leukotrienes are the most potent bronchoconstrictors known and also have pro-inflammatory effects, making them important mediators in the pathophysiology of human asthma. Early pharmacologic profiling studies have proved the existence of at least 2 cys-LT receptors in mammalian tissues, namely the type 1 cys-LT receptor and type 2 cys-LT receptor. The type 1 cys-LT receptor is a high-affinity receptor for LTD4 and the target of antagonists that are used for the management of asthma. Human CysLT1R mRNA is expressed in bronchial smooth muscle and substantially in myeloid cells, such as macrophages and mast cells. While the human CysLT2R is 38% identical to CysLT1R in amino acid sequence and it binds LTC4 and LTD4 with equal affinity. Furthermore, CysLT2R is expressed both on cells that also express CysLT1R as well as endothelial cells, cardiac Purkinje cells, adrenal medulla, and brain.
Here, we have listed all the members of the Cys-LT receptor family, including cysteinyl leukotriene receptor 1 and cysteinyl leukotriene receptor 2. To learn more information about CysLT1R and CysLT2R, please click the links below.
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