UDPglukuronosyltransferase

UDPglucuronosyltransferases (UGTs) are a superfamily of enzymes primarily responsible for the glucuronidation of a wide variety of xenobiotics and endogenous compounds. This process involves the transfer of a glucuronic acid moiety from uridine diphosphate glucuronic acid (UDPGA) to a substrate. This conjugation reaction typically increases the water solubility of the substrate, facilitating its excretion from the body, often via urine or bile.

UGTs play a crucial role in the detoxification and elimination of many drugs, environmental pollutants, and metabolic byproducts. They are involved in the metabolism of bilirubin, steroids, bile acids, and various xenobiotics, including pharmaceuticals, pesticides, and food additives. The human genome encodes for several UGT isoforms, each with distinct substrate specificities and tissue distributions. These isoforms are broadly classified into families based on their sequence homology.

Genetic variations, or polymorphisms, in UGT genes can significantly affect an individual's response to drugs and their susceptibility to certain diseases. For instance, variations in UGT1A1 are associated with differences in the metabolism of drugs like acetaminophen and irinotecan, and are implicated in conditions such as Gilbert's syndrome. Understanding the function and regulation of UGTs is therefore important for drug development, personalized medicine, and toxicology.