CysLT1

CysLT1 Receptor

The CysLT1 receptor, also known as the cysteinyl leukotriene receptor 1, is a G protein-coupled receptor (GPCR) that is primarily involved in the inflammatory response. It is one of the receptors for cysteinyl leukotrienes, which are lipid mediators derived from arachidonic acid metabolism. These leukotrienes play a significant role in conditions such as asthma, allergic rhinitis, and other inflammatory diseases.

Structure

The CysLT1 receptor is a member of the GPCR superfamily, characterized by its seven transmembrane alpha-helices. The receptor is encoded by the human gene CYSLTR1, which is located on chromosome 10q21.1. The receptor's structure allows it to interact with its ligands, the cysteinyl leukotrienes, and initiate intracellular signaling pathways.

Function

CysLT1 receptors are primarily expressed in the lungs, spleen, and peripheral blood leukocytes. They mediate the effects of leukotrienes C4, D4, and E4, which are potent bronchoconstrictors and play a crucial role in the pathophysiology of asthma and allergic reactions. Upon activation by their ligands, CysLT1 receptors trigger a cascade of intracellular events leading to increased calcium levels, smooth muscle contraction, and enhanced vascular permeability.

Clinical Significance

The CysLT1 receptor is a target for therapeutic intervention in asthma and allergic rhinitis. Antagonists of the CysLT1 receptor, such as Montelukast and Zafirlukast, are used to manage these conditions by blocking the action of leukotrienes, thereby reducing inflammation and bronchoconstriction.

Pharmacology

CysLT1 receptor antagonists are orally active drugs that bind to the receptor and inhibit its interaction with leukotrienes. These drugs are particularly useful in patients with aspirin-exacerbated respiratory disease (AERD) and exercise-induced bronchoconstriction. They are often used as an adjunct to inhaled corticosteroids in the management of chronic asthma.

Research

Ongoing research is focused on understanding the role of CysLT1 receptors in other inflammatory conditions and exploring new therapeutic agents that can modulate this receptor's activity. Studies are also investigating the genetic variations in the CYSLTR1 gene and their implications for disease susceptibility and treatment response.

Also see

• Leukotriene receptor antagonist
• Asthma
• Allergic rhinitis
• G protein-coupled receptor
• Arachidonic acid