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Objective and methods: Leukotrienes (LTs) including cysteinyl leukotrienes (CysLTs) and LTB₄ are the most potent inflammatory lipid mediators and play a central role in the pathophysiology of asthma and other inflammatory diseases. These biological molecules mediate a plethora of contractile and inflammatory responses through specific interaction with distinct G protein-coupled receptors (GPCRs). The main objective of this review is to present an overview of the biological effects of CysLTs and their receptors, along with the current knowledge of mechanisms and role of LTs in the pathogenesis of asthma. Results: CysLTs including LTC₄, LTD₄ and LTE₄ are ligands for CysLT₁ and CysLT₂ receptors, and LTB₄ is the agonist for BLT₁ and BLT₂ receptors. The role of CysLT₁ receptor is well established, and most of the pathophysiological effects of CysLTs in asthma are mediated by CysLT₁ receptor. Several …