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Leukotriene receptors as potential therapeutic targets
Takehiko Yokomizo, … , Motonao Nakamura, Takao Shimizu
Takehiko Yokomizo, … , Motonao Nakamura, Takao Shimizu
Published May 14, 2018
Citation Information: J Clin Invest. 2018;128(7):2691-2701. https://doi.org/10.1172/JCI97946.
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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 1

Structure of guinea pig BLT1 bound with a BLT antagonist, BIIL260.

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Structure of guinea pig BLT1 bound with a BLT antagonist, BIIL260.
(A) O...
(A) Overall structure of BLT1 and BIIL260 complex (35). BLT1 is presented as a rainbow-colored cartoon model, and BIIL260 is presented as pink (carbon), blue (nitrogen), and red (oxygen) spheres. (B) Mode of BIIL260 binding by BLT1. BLT1 side chains within 4 Å from BIIL260 are presented by stick models. Carbon and sulfur atoms of BLT1 are colored green and gold, respectively. The salt bridge and hydrogen bond interactions are indicated by black dashed lines. (C) Docking of LTB4 in the orthosteric binding site of BLT1. The docking study was performed with the program AutoDock 4 (184). Carbon atoms of LTB4 are colored yellow. The residues involved in the LTB4 binding shown by the mutation study (36) are presented by stick models.
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