Inhibition of phospholipase A2 as a therapeutic target

Saul Yedgar; Dov Lichtenberg; Edit Schnitzer

doi:10.1016/S1388-1981(00)00120-7

Inhibition of phospholipase A₂ as a therapeutic target

Saul Yedgar^*, Dov Lichtenberg, Edit Schnitzer

^*Corresponding author for this work

Racah Institute of Physics

Research output: Contribution to journal › Review article › peer-review

98 Scopus citations

Abstract

The hydrolysis of cell membrane phospholipids by phospholipase A₂ (PLA₂) leads to the production of numerous lipid mediators of diverse pathological conditions, mainly inflammatory diseases. These include lysophospholipids and their derivatives, and arachidonic acid and its derivatives (the eicosanoids). Both these groups of mediators are produced predominantly by the secretory PLA₂s (sPLA₂s) which hydrolyze the phospholipids of the cell surface membrane. Protection of cell membrane from these 'inflammatory enzymes' can therefore be used for the treatment of inflammatory processes. A prototype of cell-impermeable PLA₂ inhibitors, which protect the cell membrane from different sPLA₂s without affecting vital phospholipid metabolism, is presented and discussed in the present review. (C) 2000 Elsevier Science B.V.

Original language	English
Pages (from-to)	182-187
Number of pages	6
Journal	Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids
Volume	1488
Issue number	1-2
DOIs	https://doi.org/10.1016/S1388-1981(00)00120-7
State	Published - 31 Oct 2000

Keywords

Anti-inflammatory drug
Cell-impermeable PLA inhibitor
Eicosanoid
Inflammatory process
Inhibition of PLA
Phospholipase A
Secretory PLA

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10.1016/S1388-1981(00)00120-7

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title = "Inhibition of phospholipase A2 as a therapeutic target",

abstract = "The hydrolysis of cell membrane phospholipids by phospholipase A2 (PLA2) leads to the production of numerous lipid mediators of diverse pathological conditions, mainly inflammatory diseases. These include lysophospholipids and their derivatives, and arachidonic acid and its derivatives (the eicosanoids). Both these groups of mediators are produced predominantly by the secretory PLA2s (sPLA2s) which hydrolyze the phospholipids of the cell surface membrane. Protection of cell membrane from these 'inflammatory enzymes' can therefore be used for the treatment of inflammatory processes. A prototype of cell-impermeable PLA2 inhibitors, which protect the cell membrane from different sPLA2s without affecting vital phospholipid metabolism, is presented and discussed in the present review. (C) 2000 Elsevier Science B.V.",

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AB - The hydrolysis of cell membrane phospholipids by phospholipase A2 (PLA2) leads to the production of numerous lipid mediators of diverse pathological conditions, mainly inflammatory diseases. These include lysophospholipids and their derivatives, and arachidonic acid and its derivatives (the eicosanoids). Both these groups of mediators are produced predominantly by the secretory PLA2s (sPLA2s) which hydrolyze the phospholipids of the cell surface membrane. Protection of cell membrane from these 'inflammatory enzymes' can therefore be used for the treatment of inflammatory processes. A prototype of cell-impermeable PLA2 inhibitors, which protect the cell membrane from different sPLA2s without affecting vital phospholipid metabolism, is presented and discussed in the present review. (C) 2000 Elsevier Science B.V.

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KW - Eicosanoid

KW - Inflammatory process

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Inhibition of phospholipase A₂ as a therapeutic target

Abstract

Keywords

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