title: [Advances in study of metabolic activation of carboxyl-acid containing drugs by UGTs].
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.
authors.affiliation: Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
authors.forename: Tong
authors.initials: T
authors.lastname: Xie
authors.forename: Yan
authors.initials: Y
authors.lastname: Liang
authors.forename: Hai-ping
authors.initials: HP
authors.lastname: Hao
authors.forename: Lin
authors.initials: L
authors.lastname: Xie
authors.forename: Guang-ji
authors.initials: GJ
authors.lastname: Wang
mesh_terms: D001693:Biological Transport, Active; D001711:Biotransformation; D002264:Carboxylic Acids / Q000378:metabolism* / Q000633:toxicity*; D004249:DNA Damage / Q000187:drug effects; D064420:Drug-Related Side Effects and Adverse Reactions; D020719:Glucuronides / Q000378:metabolism* / Q000633:toxicity*; D014453:Glucuronosyltransferase / Q000378:metabolism*; D022781:Hepatocytes / Q000378:metabolism; D006801:Humans; D004364:Pharmaceutical Preparations / Q000378:metabolism
chemical_list: D002264:Carboxylic Acids; D020719:Glucuronides; D004364:Pharmaceutical Preparations; D014453:Glucuronosyltransferase