What do UGTs do?
UDP-glucuronosyltransferases (UGTs) are membrane-bound phase II drug-metabolizing enzymes. They catalyze the glucuronidation of substrates containing a nucleophilic O-, N-, S- group.
What is function of uridine diphosphate Glucuronosyltransferase?
The uridine diphosphate (UDP)-glucuronosyltransferases (UGT) are a family of enzymes that catalyse the covalent addition of glucuronic acid to a wide range of lipophilic chemicals.
What is UDP enzyme?
UDP-glucuronosyltransferase (UGT) enzymes comprise a superfamily of key proteins that catalyze the glucuronidation reaction on a wide range of structurally diverse endogenous and exogenous chemicals. Glucuronidation is one of the major phase II drug-metabolizing reactions that contributes to drug biotransformation.
Where is UGT located?
The bilirubin-UGT enzyme is primarily found in cells of the liver, where bilirubin glucuronidation takes place. Conjugated bilirubin is dissolved in bile, a fluid produced in the liver, and excreted with solid waste.
What happens during Glucuronidation?
Glucuronidation is a major and very frequent reaction of conjugation. It involves the transfer to the substrate of a molecule of glucuronic acid from the cofactor uridine-5′-diphospho-α-D-glucuronic acid (UDPGA).
What is UGT metabolism?
Uridine glucuronyl transferases (UGT) are a family of enzymes which play a major role in the metabolism of drugs. Glucuronidation involves the addition (or conjugation) of glucuronic acid either directly to the drug itself or to an oxidative metabolite of the drug.
What is Glucuronidation metabolism?
Glucuronidation involves the metabolism of parent compound by UDP-glucuronosyltransferases (UGTs) into hydrophilic and negatively charged glucuronides that cannot exit the cell without the aid of efflux transporters.
What enzyme converts unconjugated bilirubin?
enzyme glucuronyl transferase
In the bloodstream, unconjugated bilirubin binds to albumin to facilitate its transport to the liver. Once in the liver, glucuronic acid is added to unconjugated bilirubin by the enzyme glucuronyl transferase.
What does UGT stand for?
|Union General de Trabajadores (Socialist General Union of Workers)
|Upper Gastrointestinal Tract
What is Glucuronidation reaction?
Glucuronidation is a conjugation reaction whereby glucuronic acid, derived from cofactor UDP-glucuronic acid, is covalently linked to a substrate containing a nucleophilic functional group. The resultant metabolite, called a glucuronide, is usually excreted in bile and urine.
What kind of enzyme is UDP glucuronosyltransferase ( UGT )?
UDP-glucuronosyltransferases (UGTs) are membrane-bound phase II drug-metabolizing enzymes.7 They catalyze the glucuronidation of substrates containing a nucleophilic O-, N-, S- group. The cofactor for the UGT enzyme family is uridine-5′-diphospho-α- d -glucuronic acid (UDPGA).
How is glucuronosyl transferase related to uridine diphosphate?
Glucuronosyl transferases are a family of enzymes that catalyze the transfer of glucuronic acid from uridine diphosphate (UDP)-glucuronic acid to acceptor molecules containing hydroxyl, phenol, carboxylic acid, thiol, or amine groups (Mulder 1992; Tukey and Strassburg 2000).
Which is more polar UDPGA or glucuronosyltransferase?
The glucuronidation reaction consists of the transfer of the glucuronosyl group from uridine 5′-diphospho-glucuronic acid (UDPGA) to substrate molecules that contain oxygen, nitrogen, sulfur or carboxyl functional groups. The resulting glucuronide is more polar (e.g. hydrophilic) and more easily excreted than the substrate molecule.
Which is the substrate of the UGT in UDPGA?
UGTs are responsible for the metabolism of many xenobiotics (and endogenous substrates). Substrates of UGTs include aliphatic alcohols, phenols, carboxylic acids, thiols, and amines. The GA in UDPGA is in the α configuration at the C1 atom.