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Mechanism of action of anti-inflammatory drugs: an overview

  • Chapter
Selective COX-2 Inhibitors

Abstract

Among the many mediators of inflammation, the prostaglandins (PGs) are of great importance. They are released by almost any type of chemical or mechanical stimulus. The key enzyme in their synthesis is prostaglandin endoperoxide synthase (PGHS) or cyclooxygenase (COX) which possesses two catalytic sites. The first, a cyclooxygenase active site, converts arachidonic acid to the endoperoxide PGG2. The second, a peroxidase active site, then converts the PGG2 to another endoperoxide PGH2. PGH2 is further processed by specific isomerases to form PGs, prostacyclin and thromboxane A2. Of the PGs, PGE2 and prostacyclin are the main inflammatory mediators. Cyclooxygenase activity has long been studied in preparations from sheep seminal vesicles and a purified, enzymatically-active COX was isolated in 19761. We now know that COX exists in at least two isoforms, COX-1 and COX-2.

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  1. J. R. Vane
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  1. The William Harvey Research Institute, Saint Bartholomew’s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, UK

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Vane, J.R., Botting, R.M. (1998). Mechanism of action of anti-inflammatory drugs: an overview. In: Vane, J., Botting, J. (eds) Selective COX-2 Inhibitors. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-4872-6_1

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