Secretory phospholipase A2 enzymes as pharmacological targets for treatment of disease.

Abstract:

:Phospholipase A2 (PLA2) cleave phospholipids preferentially at the sn-2 position, liberating free fatty acids and lysophospholipids. They are classified into six main groups based on size, location, function, substrate specificity and calcium requirement. These classes include secretory PLA2 (sPLA2), cytosolic (cPLA2), Ca(2+)-independent (iPLA2), platelet activating factor acetylhydrolases (PAF-AH), lysosomal PLA2 (LyPLA2) and adipose specific PLA2 (AdPLA2). It is hypothesized that PLA2 can serve as pharmacological targets for the therapeutic treatment of several diseases, including cardiovascular diseases, atherosclerosis, immune disorders and cancer. Special emphasis has been placed on inhibitors of sPLA2 isoforms as pharmacological moieties, mostly due to the fact that these enzymes are activated during inflammatory events and because their expression is increased in several diseases. This review focuses on understanding how sPLA2 isoform expression is altered during disease progression and the possible therapeutic interventions to specifically target sPLA2 isoforms, including new approaches using nano-particulate-based strategies.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Quach ND,Arnold RD,Cummings BS

doi

10.1016/j.bcp.2014.05.022

subject

Has Abstract

pub_date

2014-08-15 00:00:00

pages

338-48

issue

4

eissn

0006-2952

issn

1873-2968

pii

S0006-2952(14)00314-1

journal_volume

90

pub_type

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