Advances in study of metabolic activation of carboxyl-acid containing drugs by UGTs.
- Author:
Tong XIE
1
;
Yan LIANG
;
Hai-ping HAO
;
Lin XIE
;
Guang-ji WANG
Author Information
1. Key Lab of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China.
- Publication Type:Journal Article
- MeSH:
Biological Transport, Active;
Biotransformation;
Carboxylic Acids;
metabolism;
toxicity;
DNA Damage;
drug effects;
Drug-Related Side Effects and Adverse Reactions;
Glucuronides;
metabolism;
toxicity;
Glucuronosyltransferase;
metabolism;
Hepatocytes;
metabolism;
Humans;
Pharmaceutical Preparations;
metabolism
- From:
Acta Pharmaceutica Sinica
2009;44(11):1193-1199
- CountryChina
- Language:Chinese
-
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.
