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Caco-2 cells are a widely used model in drug development to study intestinal drug transport and metabolism. Recently, serotonin (5-hydroxytryptamine, 5-HT) has been characterized as a highly selective substrate of human UDP-glucuronosyltransferase UGT1A6 [Krishnaswamy S, Duan SX, von Moltke LL, Greenblatt DJ, Court MH. Validation of serotonin (5-hydroxytryptamine) as an in vitro substrate probe for...
UDP-glucuronosyltransferases (UGTs) represent major phase II enzymes of drug metabolism which are regulated in a tissue-specific manner by endogenous and environmental factors. Among the latter, aryl hydrocarbon receptor (AhR) agonists such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and phenolic antioxidants such as tert-butylhydroquinone (tBHQ) are known to induce the expression of human UGT1A6...
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