The Role of Uptake and Efflux Transporters in the Disposition of Glucuronide and Sulfate Conjugates.

ABSTRACT: Glucuronidation and sulfation are the most typical phase II metabolic reactions of drugs. The resulting glucuronide and sulfate conjugates are generally considered inactive and safe. They may, however, be the most prominent drug-related material in the circulation and excreta of humans. The glucuronide and sulfate metabolites of drugs typically have limited cell membrane permeability and subsequently, their distribution and excretion from the human body requires transport proteins. Uptake transporters, such as organic anion transporters (OATs and OATPs), mediate the uptake of conjugates into the liver and kidney, while efflux transporters, such as multidrug resistance proteins (MRPs) and breast cancer resistance protein (BCRP), mediate expulsion of conjugates into bile, urine and the intes

SUBMITTER: Jarvinen E 

PROVIDER: S-EPMC8793843 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature