Target intelligence / Profile preview

Cysteinyl Leukotriene Receptor 2 (CysLT2)

Target
CysLT2
Molecular classification
G protein–coupled receptor, GPCR, Leukotriene receptor
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Overview

Cysteinyl Leukotriene Receptor 2 (CysLT2) is a G protein-coupled receptor that belongs to the leukotriene receptor family. It is activated by cysteinyl leukotrienes, primarily LTD4, LTC4, and LTE4, with LTD4 and LTC4 having similar potency. CysLT2 is expressed in various tissues including the heart, brain, adrenal glands, vascular endothelial cells, and airway epithelial cells. It plays a role in inflammation by modulating smooth muscle contraction, vascular permeability, and leukocyte activation. Its activation exacerbates vascular permeability and postischemia/reperfusion injury. A major challenge is the lack of selective antagonists for research and therapeutic use, limiting the understanding of its precise role compared to CysLT1.

02

Mechanism of action

Gq alpha subunit protein coupling leading to downstream signaling pathways (e.g., contraction or increased permeability)

03

Biological functions

Signal transductionModulates smooth muscle contractionModulates vascular permeabilityModulates leukocyte activationMediates effects of cysteinyl leukotrienes involved in inflammation
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Disease associations

Inflammatory diseasesCardiovascular diseaseIschemia/reperfusion injury
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Safety considerations

Lack of highly selective antagonists for clinical or research useExacerbation of vascular permeability and postischemia/reperfusion injury

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