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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Advances in Inducible Cyclooxygenase (COX-2) Inhibition.

Author(s): Xavier de Leval, Jacques Delarge, Fabian Somers, Pascal de Tullio, Yves Henrotin, Bernard Pirotte and Jean-Michel Dogne

Volume 7, Issue 10, 2000

Page: [1041 - 1062] Pages: 22

DOI: 10.2174/0929867003374417

Price: $65

Abstract

Cyclooxygenase is the key enzyme in the biosynthesis of prostanoids, biologically active substances that are involved in several physiological processes but also in pathological conditions such as inflammation. Since ten years now, it is well known that this enzyme exists under two forms: a constitutive (COX-1) and an inducible form (COX-2). Both enzymes are sensitive to inhibition by conventional nonsteroidal antiinflammatory drugs (NSAIDs). Observations that COX-1, involved in several homeostatic processes, played a housekeeping role while COX-2 expression was associated with inflammation and other pathologies such as cancer proliferation have led to the development of COX-2 selective inhibitors in order to reduce the classical side-effects, of which gastric irritation is the most common, associated with the use of conventional NSAIDs.

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