cysteinyl leukotriene receptor 1 (CysLTR1, cysteinyl leukotriene D4 receptor, LTD4 receptor, HG55, HMTMF81)
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Function
- receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with & without asthma
- stimulation by LTD4 results in contraction & proliferation of smooth muscle, edema, eosinophil migration & damage to the mucus layer in the lung
- this response is mediated via a G-protein that activates a phosphatidylinositol-Ca+2 second messenger system
- the rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4
Structure
belongs to the G-protein coupled receptor 1 family
Compartment
Expression
- widely expressed, with highest levels in spleen & peripheral blood leukocytes
- lower expression in several tissues, such as lung (mostly in smooth muscle bundles & alveolar macrophages), placenta, small intestine, pancreas, colon & heart
Pharmacology
- selective antagonists, such as montelukast (singulair), zafirlukast (accolate) & pranlukast (Onon), are used in the treatment of the asthma