UGT2B7

UGT2B7 (UDP-Glucuronosyltransferase-2B7) is a phase II is_associated_with::metabolism isoenzyme found to be active in the is_associated_with::liver, is_associated_with::kidneys, epithelial cells of the lower is_associated_with::gastrointestinal tract and also has been reported in the is_associated_with::brain. In humans, UDP-Glucuronosyltransferase-2B7 is encoded by the UGT2B7 is_associated_with::gene.

Function
The UGTs serve a major role in the conjugation and subsequent elimination of potentially toxic is_associated_with::xenobiotics and endogenous compounds. UGT2B7 has unique specificity for 3,4-is_associated_with::catechol is_associated_with::estrogens and is_associated_with::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 is_associated_with::endoplasmic reticulum and nuclear membranes of cells. Its function is to catalyse the conjugation of a wide variety of lipophilic is_associated_with::aglycon substrates with is_associated_with::glucuronic acid, using is_associated_with::uridine diphosphate glucuronic acid.

Together with is_associated_with::UGT2B4, UGT2B7 is capable of glucosidation of is_associated_with::hyodesoxycholic acid in the liver, but, unlike the 2B4 isoform, 2B7 is also able to glucuronidate various is_associated_with::steroid hormones (is_associated_with::androsterone, is_associated_with::epitestosterone) and is_associated_with::fatty acids. It is also able to conjugate major classes of drugs such as analgesics (is_associated_with::morphine), carboxylic nonsteroidal anti-inflammatory drugs (is_associated_with::ketoprofen), and anticarcinogens (all-trans is_associated_with::retinoic acid). UGT2B7 is the major enzyme isoform for the metabolism of is_associated_with::morphine to the main metabolites, is_associated_with::morphine-3-glucuronide (M3G) which has no analgesic effect and is_associated_with::morphine-6-glucuronide (M6G), which has analgesic effects less potent than morphine. As a consequence, altered UGT2B7 activity can significantly affect both the effectiveness and side-effects of morphine, as well as some related opiate drugs.