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Leukotriene receptors as potential therapeutic targets
Takehiko Yokomizo, … , Motonao Nakamura, Takao Shimizu
Takehiko Yokomizo, … , Motonao Nakamura, Takao Shimizu
Published July 2, 2018; First published May 14, 2018
Citation Information: J Clin Invest. 2018;128(7):2691-2701. https://doi.org/10.1172/JCI97946.
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Category: Review Series

Leukotriene receptors as potential therapeutic targets

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Abstract

Leukotrienes, a class of arachidonic acid–derived bioactive molecules, are known as mediators of allergic and inflammatory reactions and considered to be important drug targets. Although an inhibitor of leukotriene biosynthesis and antagonists of the cysteinyl leukotriene receptor are clinically used for bronchial asthma and allergic rhinitis, these medications were developed before the molecular identification of leukotriene receptors. Numerous studies using cloned leukotriene receptors and genetically engineered mice have unveiled new pathophysiological roles for leukotrienes. This Review covers the recent findings on leukotriene receptors to revisit them as new drug targets.

Authors

Takehiko Yokomizo, Motonao Nakamura, Takao Shimizu

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Figure 2

Signaling via CysLT1, CysLT2, GPR17, GPR99, and P2Y12.

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Signaling via CysLT1, CysLT2, GPR17, GPR99, and P2Y12.
Synthetic antagon...
Synthetic antagonists for each receptor are given in red text. Ligands and relative affinities are described adjacent to their respective receptor. GPR17 is a negative regulator for CysLT1. Shown below each receptor is its downstream coupling to Gi/o and adenylyl cyclase (AC) and/or Gq/11 and phospholipase Cβ (PLCβ).
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