Uridine 5'-diphospho-glucuronosyltransferase (UGT)

Uridine 5'-diphospho-glucuronosyltransferase (UGT) refers to a superfamily of membrane-bound glycosyltransferase enzymes primarily responsible for the glucuronidation reaction, a key Phase II metabolic process. UGTs transfer a glucuronic acid group from UDP-glucuronic acid to various substrates containing oxygen, nitrogen, sulfur, or carboxyl functional groups, including many drugs, toxins, dietary substances, and endogenous molecules such as bilirubin and steroid hormones[1][2][4][6]. This process increases substrate polarity and water solubility, facilitating excretion mainly via urine and bile and enabling the detoxification and clearance of potentially harmful substances from the body[1][2][6]. The human UGTs are divided into several families and subfamilies, most notably UGT1 and UGT2, which feature genetic polymorphisms that influence individual responses to drugs and susceptibility to toxicity[4][7]. Clinically, UGT enzymes play a significant role in drug metabolism, affecting the efficacy and safety of numerous therapeutic agents, including opioids, analgesics, anticonvulsants, antiviral drugs, and more[4][5]. Genetic defects in UGT enzymes (such as UGT1A1) can result in conditions like Crigler-Najjar syndrome and are also implicated in variations in drug response and toxicity[7]. UGTs are further implicated in cancer biology, both by inactivating drug therapies (leading to drug resistance) and potentially influencing cancer progression[5]. Species differences in UGT enzyme activity account for significant variations in drug safety profiles (e.g., cats lack certain UGTs, leading to unique toxicities)[1][4]. Pharmacogenetic testing of UGT genes is increasingly important for predicting drug response, tailoring therapies, and monitoring for adverse reactions[5][7].

Other names

glucuronosyltransferaseUDP-glucuronosyltransferaseUDPGTglucuronyltransferaseUDP-glucuronyl transferaseUDP-GT

Glucuronidation to increase solubility & elimination, Inactivation of drugs, Detoxification of endogenous and exogenous compounds