Volume 644 of the series Methods in Molecular Biology pp 67-90


Study of Inhibitors of the PGH Synthases for which Potency Is Regulated by the Redox State of the Enzymes

  • Olivier BoutaudAffiliated withDepartment of Pharmacology, Vanderbilt University
  • , John A. OatesAffiliated withDepartments of Pharmacology and Medicine, Vanderbilt University

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Aspirin, salicylic acid, and acetaminophen are examples of drugs that inhibit the PGH synthases (cyclooxygenases) with potencies that vary remarkably between different cells. This results from the fact that the inhibitory action of these drugs is regulated by redox cycling of the enzymes, which is determined by the concentration of hydroperoxides in the enzyme proximity. The potency of these drugs is greatest in the presence of low concentrations of hydroperoxides. Accordingly, analysis of the action of these inhibitors requires consideration of assay conditions that take into account the factors that control hydroperoxide concentrations, both in studies with purified enzymes and in cells.

Key words

Cyclooxygenase Assay Hydroperoxide Inhibitor Acetaminophen Aspirin Salicylic acid