Inhibitors of Secretory Phospholipase A2 Group IIA

Reid, Robert C. (2005) Inhibitors of Secretory Phospholipase A2 Group IIA. Current medicinal chemistry, 12 25: 3011-3026. doi:10.2174/092986705774462860


Author Reid, Robert C.
Title Inhibitors of Secretory Phospholipase A2 Group IIA
Journal name Current medicinal chemistry   Check publisher's open access policy
ISSN 0929-8673
Publication date 2005-12-01
Year available 2005
Sub-type Critical review of research, literature review, critical commentary
DOI 10.2174/092986705774462860
Volume 12
Issue 25
Start page 3011
End page 3026
Total pages 16
Place of publication Oak Park, IL
Publisher Bentham Science Publishers
Language eng
Subject 0304 Medicinal and Biomolecular Chemistry
Abstract Phospholipases A2 cleave membrane phospholipids to release arachidonic acid, the precursor to a large family of pro-inflammatory eicosanoids including prostaglandins and leukotrienes that have been proven to exacerbate numerous diseases that have an inflammatory component. Current therapies include NSAIDs' that inhibit cyclooxygenases (COX-1, COX-2) but have no effect on the production of leukotrienes or platelet activating factor (PAF). Inhibitors of PLA2 therefore offer the potential to block production of a more complete set of inflammatory substances through blockade at the onset of the cascade of reactions that follow arachidonic acid release. Many potent, bioavailable and selective inhibitors of human sPLA2 group IIA have been available for more than a decade and have provided compelling support for a causative role of sPLA2 group IIA in numerous studies involving animal models of inflammatory diseases. However, the true value of sPLA2 inhibitors for the treatment of human diseases has had to await phase II clinical trials which have only been completed in the last two years. This review presents the structurally diverse array of available sPLA2 group IIA inhibitors, their associated biological activity in animal models, and evaluation of therapeutic potential in phase II clinical trials in humans.
Keyword phospholipase a2 inhibitor2
pla2
spla2
secretory pla2
anti-inflammatory
inflammation
clinical trial
Q-Index Code C1
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Excellence in Research Australia (ERA) - Collection
Institute for Molecular Bioscience - Publications
 
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Created: Tue, 20 Jan 2009, 23:53:47 EST by Ms Karen Naughton on behalf of Institute for Molecular Bioscience