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
Current Drug Targets
Title:Leukotriene C4 Synthase: Upcoming Drug Target For Inflammation
Volume: 13 Issue: 8
Author(s): Nisha S. Devi and Mukesh Doble
Affiliation:
Keywords: Asthma, anti-inflammatory drugs, inflammation, inhibitors, leukotriene C4 synthase, 5-lipoxygenase, antigen attack, cysteinyl leukotrienes, bronchoconstriction, prostaglandins
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.
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Cite this article as:
S. Devi Nisha and Doble Mukesh, Leukotriene C4 Synthase: Upcoming Drug Target For Inflammation, Current Drug Targets 2012; 13 (8) . https://dx.doi.org/10.2174/138945012802009053
DOI https://dx.doi.org/10.2174/138945012802009053 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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