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  • Title: [Advances in study of metabolic activation of carboxyl-acid containing drugs by UGTs].
    Author: Xie T, Liang Y, Hao HP, Xie L, Wang GJ.
    Journal: Yao Xue Xue Bao; 2009 Nov; 44(11):1193-9. PubMed ID: 21355318.
    Abstract:
    The metabolic transformation of the drugs containing carboxylic acid groups can lead to the formation of acyl glucuronide metabolites through catalysis by glucuronosyltransferase, and produce pro-acyl glucuronide intermediate metabolites with electronic activity. Then, protein or DNA adducts appeared after a series of non-enzyme or enzyme reactions. These adducts would change the protein activity and potentially lead to idiosyncratic and genotoxicity. In this paper, we discussed the chemical activity, drug-induced mechanisms, distribution and toxicity resulting from this metabolic activation for these drugs, and stated the status and prospects of research in this field.
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