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Overview
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Phase II metabolism, also known as the binding reaction, refers to the reaction in which phase I metabolites or prototype drugs combine with endogenous small molecules via phase II enzymes, leading to the reduction of toxicity, activity, or polarity of prodrugs. In phase II metabolism, the most common reaction is glucuronidation, during which the uridine diphosphate glucuronic acid (UDPGA) is bound to the prodrug via catalyzation by glucuronyl transferase in microsomes. The glucuronide formed increases water-solubility of metabolites to enhance the excretion. The phase II metabolic system can be reconstructed by combination of liver microsomes and UGT and used to study phase II metabolic stability of drug candidates in vitro.
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Overview