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Current Drug Targets

Editor-in-Chief

ISSN (Print): 1389-4501
ISSN (Online): 1873-5592

Leukotriene C4 Synthase: Upcoming Drug Target For Inflammation

Author(s): Nisha S. Devi and Mukesh Doble

Volume 13 , Issue 8 , 2012

Page: [1114 - 1125] Pages: 12

DOI: 10.2174/138945012802009053

Price: $65

Abstract

Leukotrienes are important mediators of pain and inflammation and they are produced in the arachidonic acid pathway via 5-lipoxygenase. They have been shown to have important roles in pyresis following antigen attack and in aspirin- intolerant asthma. They promote inflammation processes including eosinophil migration, increase in vascular permeability and bronchoconstriction. Hence, targeting the enzymes involved in the synthesis of these mediators can lead to the development of novel anti-inflammatory drugs. However, no drugs have yet been developed targeting leukotriene C4 synthase, a key enzyme leading to the synthesis of cysteinyl leukotrienes. The recent elucidation of its crystal structure now opens up the possibility of drugs against it. The inhibitors developed for this enzyme until now and the structural features responsible for their activity are discussed in this review. This understanding could lead to the design of new chemical entities.

Keywords: Asthma, anti-inflammatory drugs, inflammation, inhibitors, leukotriene C4 synthase, 5-lipoxygenase, antigen attack, cysteinyl leukotrienes, bronchoconstriction, prostaglandins


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