UGT2B7
Description
The UGT2B7 (UDP glucuronosyltransferase family 2 member B7) is a protein-coding gene located on chromosome 4.
UGT2B7 (UDP-Glucuronosyltransferase-2B7) is a phase II metabolism isoenzyme found to be active in the liver, kidneys, epithelial cells of the lower gastrointestinal tract and also has been reported in the brain. In humans, UDP-Glucuronosyltransferase-2B7 is encoded by the UGT2B7 gene.
== Function == The UGTs serve a major role in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. UGT2B7 has unique specificity for 3,4-catechol estrogens and estriol, suggesting that it may play an important role in regulating the level and activity of these potent estrogen metabolites. This enzyme is located on the endoplasmic reticulum and nuclear membranes of cells. Its function is to catalyse the conjugation of a wide variety of lipophilic aglycon substrates with glucuronic acid, using uridine diphosphate glucuronic acid. Together with UGT2B4, UGT2B7 is capable of glucosidation of hyodesoxycholic acid in the liver, but, unlike the 2B4 isoform, 2B7 is also able to glucuronidate various steroid hormones (androsterone, epitestosterone) and fatty acids. It is also able to conjugate major classes of drugs such as analgesics (morphine), carboxylic nonsteroidal anti-inflammatory drugs (ketoprofen), and anticarcinogens (all-trans retinoic acid). UGT2B7 is the major enzyme isoform responsible for the metabolism of morphine, codeine, norcodeine and other opiates to their corresponding 3- and 6- glucuronides. For example, morphine metabolism produces morphine-3-glucuronide (M3G) which has no analgesic effect and morphine-6-glucuronide (M6G), which has analgesic effects more potent than morphine.
UGT2B7 is a UDP-glucuronosyltransferase enzyme that plays a key role in phase II biotransformation reactions, where it conjugates lipophilic substrates with glucuronic acid. This conjugation increases the water solubility of the metabolite, making it easier to excrete through urine or bile. UGT2B7 is essential for eliminating and detoxifying various substances including drugs, xenobiotics, and endogenous compounds. It is known to catalyze the glucuronidation of steroid hormones like androgens (epitestosterone, androsterone) and estrogens (estradiol, epiestradiol, estriol, catechol estrogens). Additionally, UGT2B7 regulates the levels of retinoic acid, a vitamin A metabolite involved in essential cellular processes like apoptosis, growth, differentiation, and embryonic development. It also contributes to bile acid detoxification by catalyzing the glucuronidation of bile acid substrates, which are essential for lipid absorption. Furthermore, UGT2B7 is involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist drugs losartan, caderastan, and zolarsatan, which inhibit the effects of angiotensin II. Finally, it also metabolizes mycophenolate, an immunosuppressive agent.
UGT2B7 is also known as UDPGT 2B7, UDPGT 2B9, UDPGT2B7, UDPGTH2, UDPGTh-2, UGT2B9.
