Lack of covalent modification of prostaglandin synthetase (cyclo-oxygenase) by indomethacin |
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Authors: | Nancy Stanford Gerald J Roth TY Shen Philip W Majerus |
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Institution: | 2. Merck, Sharp & Dohme Research Laboratories, Rahway, N.J. 07065, USA |
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Abstract: | We have previously shown that aspirin irreversibly inhibits prostaglandin synthetase (cyclo-oxygenase) by acetylating the active site of the enzyme. By utilizing 14C-labeled indomethacin and a close analogue, we now show that indomethacin, unlike aspirin, does not covalently modify cyclo-oxygenase. Furthermore, indomethacin binding to the enzyme may be reversible since even though indomethacin can inhibit acetylation by aspirin, when enzyme inhibited by indomethacin (1 μM) is treated with 200 μM aspirin 3 times for 1 hour each, complete acetylation of cyclo-oxygenase is achieved. |
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