Biochem/physiol Actions
COX-2 catalyzes the conversion of arachidonic acid to prostaglandin H2 (the first step in the biosynthesis of prostaglandins, thromboxanes, and prostacyclins). It is the inducible form of cyclooxygenase, induced by phorbol esters, lipopolysaccharides, and cytokines. COX-2 is upregulated in the neovasculature of malignant tumors. Inhibition of COX-2 with nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with decreased tumor growth.
Other Notes
Tagged with a six-residue histidine sequence near the N-terminus.
Substrates
KM for arachidonate = 6.5 μM. Exhibits activity and sensitivity to NSAIDs similar to the non-tagged enzyme.
Unit Definition
One unit consumes one nanomole of oxygen per minute at 37 °C in 0.1 M Tris-HCl buffer, pH 8, containing 100 μM arachidonate, 5 mM EDTA, 2 mM phenol, and 1 μM hematin.
Physical form
Solution in 80 mM Tris-HCl, pH 8, with 0.1% TWEEN® 20 and 300 μM diethyldithiocarbamate.