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The Application of Rational Design on Phospholipase A2 Inhibitors

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The phospholipase A2 (PLA2) superfamily consists of different groups of enzymes which are characterized by their ability to catalyze the hydrolysis of the sn-2 ester bond in a variety of phospholipid molecules. The products of PLA2s activity play divergent roles in a variety of physiological processes. There are four main types of PLA2s: the secreted PLA2s (sPLA2s), the cytosolic PLA2s (cPLA2s), the calcium-independent PLA2s (iPLA2) and the lipoprotein-associated PLA2s (LpPLA2s). Various potent and selective PLA2 inhibitors have been reported up to date and have provided outstanding support in understanding the mechanism of action and elucidating the function of these enzymes. The current review focuses on the implementation of rational design through computer-aided drug design (CADD) on the discovery and development of new PLA2 inhibitors.

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Keywords: Computer-aided drug design; LpPLA2s; PLA2; enzymes; hydrolysis; iPLA2; inhibitors; phospholipases A2; phospholipid; rational design

Document Type: Research Article

Publication date: 01 June 2011

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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