What does UGT2B7 do?
The isoenzyme UGT2B7 is the major enzyme responsible for glucuronidation of morphine while UGT1A1 plays a minor role. There are conflicting reports regarding association between UGT2B7 polymorphism and metabolism of morphine.
Where is UGT enzyme located?
the liver
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 is the function of glucuronidation?
Glucuronidation, a conjugation reaction, is thought to protect the liver by both reducing hepatic BA toxicity and increasing their urinary elimination.
What are UGT enzymes?
The UDP-glucuronosyltransferases (UGTs) are a superfamily of enzymes that catalyze the conjugation of glucuronic acid to molecules primarily to facilitate systemic elimination (Radominska-Pandya et al., 1999).
What is a CYP substrate?
substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body.
What is glucuronidation metabolism?
n. a metabolic process by which drugs or other substances are combined with glucuronic acid to form more water-soluble compounds, which are more readily excreted by the kidneys or in bile. Glucuronidation is the most prevalent of the Phase II reactions of drug metabolism.
What is glucuronidation and sulfation?
Sulfation and glucuronidation are the principal metabolic pathways of flavonoids, and extensive phase II metabolism is the main reason for their poor bioavailabilities.
What is CYP450 3A4 substrate?
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14. 13.97) is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.
What is a CYP3A4 substrate?
What is CYP3A4 metabolism?
CYP3A4 is responsible for the metabolism of more than 50% of medicines. CYP3A4 activity is absent in new-borns but reaches adult levels at around one year of age. The liver and small intestine have the highest CYP3A4 activity.
What is sulfation in biology?
Sulfation is an important pathway of metabolism for a range of endogenous compounds including steroid hormones, bile acids, neurotransmitters, and small peptides. Xenobiotics also undergo conjugation by sulfation, which generally, but not exclusively, leads to reduced biological activity.
What is the function of Glucuronidation?
What does UGT2B7 stand for?
In humans, UDP-Glucuronosyltransferase-2B7 is encoded by the UGT2B7 gene. The UGTs serve a major role in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
What is the structure of the human UGT enzyme?
No structure of a full human UGT enzyme has been determined yet, however Miley et al. resolved a partial UGT2B7 structure of the C-terminal portion showing two dimeric domains with Rossman-like folds in complex.
Is human UGT2B7 involved in the O-glucuronidation of chloramphenicol?
“Identification of human UGT2B7 as the major isoform involved in the O-glucuronidation of chloramphenicol”. Drug Metabolism and Disposition. 38 (3): 368–75. doi: 10.1124/dmd.109.029900.
Is glucuronidation activity of UGT2B7 affected by polymorphic variants?
UGT2B7 is considered to be a highly polymorphic gene. Various research efforts have investigated the potential effect of these polymorphic variants on glucuronidation activity of UGT2B7 and especially its clearance of administered drugs, including anticancer therapies.