1997
DOI: 10.1517/13543784.6.3.279
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Phospholipase A2 inhibitors in development

Abstract: To date, three isoforms of phospholipase A2 (PLA2) have been identified. Of these, the two Ca2+-dependent isoforms, secretory (sPLA2) and cytosolic phospholipase A2 (cPLA2), are targets for new anti-inflammatory drugs. The catalytic mechanisms and functions of the third isoform, Ca2+-independent cytosolic phospholipase A2 (iPLA2), are unknown at present. sPLA2 and cPLA2 are both implicated in the release of arachidonic acid and prophlogistic lipid mediators. However, recent findings provide evidence that cPLA2… Show more

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Cited by 26 publications
(18 citation statements)
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“…Based on the central role of lipid mediators in the inflammatory processes, the potential value of controlling phospholipid metabolism through PLA2 inhibition has always been acknowledged [30]. Numerous compounds have been proposed as inhibitors of various sPLA2.…”
Section: Introductionmentioning
confidence: 99%
“…Based on the central role of lipid mediators in the inflammatory processes, the potential value of controlling phospholipid metabolism through PLA2 inhibition has always been acknowledged [30]. Numerous compounds have been proposed as inhibitors of various sPLA2.…”
Section: Introductionmentioning
confidence: 99%
“…Prostaglandins, leukotrienes, lysophospholipids and the PAF are potent mediators of inflammation [1][2][3]. Thus, inhibition of PLA 2 is considered as an interesting target for the design of new anti-inflammatory drugs [4][5][6][7][8].…”
Section: Introductionmentioning
confidence: 99%
“…Inhibitors of phospholipases A 2 have been reviewed in the literature on many occasions [49][50][51][52][53][54][55][56][57]; the most recent comprehensive review being that of Tibes and Friebe in 1997 [58]. It is the intent of this review to provide an update of small molecule inhibitors of human Type II s-PLA 2 since the time of the Tibes and Friebe report, that are in clinical trials or in late-stage development as potential anti-inflammatory agents.…”
Section: Introductionmentioning
confidence: 99%