Recent advances in inducible cyclooxygenase (COX-2) inhibition

X de Leval, J Delarge, F Somers, P de Tullio, Y Henrotin, B Pirotte, J M Dogné

Research output: Contribution to journalArticlepeer-review

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 anti-inflammatory 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.
Original languageEnglish
Pages (from-to)1041-62
Number of pages22
JournalCurrent Medicinal Chemistry
Volume7
Issue number10
Publication statusPublished - Oct 2000

Keywords

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal
  • Clinical Trials as Topic
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Enzyme Induction
  • Enzyme Inhibitors
  • Humans
  • Isoenzymes
  • Membrane Proteins
  • Molecular Structure
  • Prostaglandin-Endoperoxide Synthases
  • Prostaglandins
  • Substrate Specificity

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