Prostaglandin-endoperoxide synthase 1 (COX-1) and Prostaglandin-endoperoxide synthase 2 (COX-2) (COX-1 (PTGS1), COX-2 (PTGS2))

Cyclooxygenase-1 and cyclooxygenase-2 are enzymes central to the conversion of arachidonic acid to prostaglandins and thromboxanes, key mediators of inflammation, pain, fever, and several physiological homeostatic functions. COX-1 is constitutively expressed in most tissues and supports physiological processes such as gastric protection and platelet aggregation; COX-2 is normally inducible in response to inflammation and other stimuli and is heavily implicated in pathological conditions, including cancer. Both are homodimeric proteins with highly similar structures, although their active sites differ sufficiently to allow selective drug targeting, which is the basis for the development of COX-2 selective inhibitors. Inhibition of these enzymes underlies both the therapeutic efficacy and notable toxicity profiles of nonsteroidal anti-inflammatory drugs.

Other names

COX-1PTGS1prostaglandin G/H synthase 1prostaglandin-endoperoxide synthetase 1COX-2PTGS2prostaglandin G/H synthase 2prostaglandin-endoperoxide synthetase 2

Inhibition of cyclooxygenase activity (prevents prostaglandin synthesis from arachidonic acid) NSAIDs: nonselective inhibition (both COX-1 and COX-2) COX-2 inhibitors: selective inhibition of COX-2