Study of inhibitors of the PGH synthases for which potency is regulated by the redox state of the enzymes

Methods in Molecular Biology
Olivier Boutaud, John A Oates

Abstract

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.

Citations

Nov 5, 2013·World Journal of Gastroenterology : WJG·Jing LuChang-You Jiang
Nov 22, 2011·Expert Opinion on Therapeutic Patents·Deniz EkinciÖmer İrfan Küfrevioğlu
Sep 16, 2011·Obesity Reviews : an Official Journal of the International Association for the Study of Obesity·F SantilliG Davì

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