Concept explainers
Interpretation:
The mechanisms by which NSAIDs inhibit cyclooxygenase-2 enzyme should be explained using the active model for the enzyme.
Concept Introduction:
Cyclooxygenase enzyme catalyzes the biosynthesis of prostaglandins by catalyzing simultaneous oxidation and cyclization of arachidonic acid. Prostaglandin enhances inflammation in animal tissues. The first step in the synthesis of prostaglandin is bis-oxygenation of arachidonate to prostaglandin PGG2. Then it is reduced to PGH2in a peroxide reaction. Both above reactions are catalyzed by cyclooxygenase. This enzyme can be inhibited by nonsteroidal anti-inflammatory drugs (NSAIDs). Examples for anti inflammatory drugs are Aspirin, ibuprofen, flurbiprofen and acetaminophen. There are two forms of cyclooxygenase. COX-1 carries normal physiological production of prostaglandins. COX-2 induced by cytokines, mitogens and endotoxins and produce prostaglandin in inflammation. Traditional NSAIDs inhibit both isozymes of the enzyme. But COX-2 selective inhibitors preferentially inhibit COX-2.
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- BiochemistryBiochemistryISBN:9781305577206Author:Reginald H. Garrett, Charles M. GrishamPublisher:Cengage Learning