作者: Adarsh Gandhi , Romi Ghose
DOI: 10.5772/28200
关键词: Biochemistry 、 Sulfation 、 Sulfotransferase 、 Detoxification 、 Metabolism 、 Glucuronidation 、 CYP3A4 、 Glutathione 、 Drug metabolism 、 Chemistry
摘要: Drug metabolism can either lead to detoxification, bio-inactivation and/or elimination of the drug from body. Metabolism be broadly categorized into phases I and II. Phase metabolizing enzymes (DMEs) primarily comprise Cytochrome (CYP) 450 family enzymes. CYP3A4 is most common isoform expressed in human liver intestine accounting for ~30-60% CYPs (Nebert & Russell, 2002) More than 50% currently marketed drugs are metabolized by humans (Guengerich, 1999). II consists conjugation reactions forming polar metabolites leading enhanced excretion. include glucuronidation (Uridine 5'-diphosphoglucuronosyltransferase, UGT) sulfation (Sulfotransferase, SULT), methylation (Methyltransferase), glutathione (Glutathione S-transferase, GST), etc. (Jancova et al., 2010; Meyer, 1996).