What are UGT inhibitors?
Glucuronidation caused by uridine 5′-diphospho-glucuronosyltransferases (UGT) is an important pathway for drug metabolism in humans and other mammals. The inhibition of UGT, although less often observed than CYP inhibition, is a clinically significant form of drug-drug interactions and may lead to toxicity.
What are UGT enzymes?
UDP-glucuronosyltransferase (UGT) enzymes catalyze the attachment of a glucuronic acid moiety to various drugs and other xenobiotics, as well as to endogenous compounds such as bilirubin. This conjugation promotes their excretion.
Where are UGT enzymes found?
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 are UGT substrate drugs?
Substrates. Estradiol (UGT1A1), sulindac sulfone (UGT1A3), trifluoperazine (UGT1A4), naphthol (UGT1A6), propofol (UGT1A9), naloxone (UGT2B7)
What is UGT?
Uridine 5′-diphospho-glucuronosyltransferase (UDP-glucuronosyltransferase, UGT) is a microsomal glycosyltransferase (EC 2.4. 1.17) that catalyzes the transfer of the glucuronic acid component of UDP-glucuronic acid to a small hydrophobic molecule. This is a glucuronidation reaction.
What do you mean by UGT?
Uridine diphosphate-glucuronyltransferase (UGT) is one kind of phase 2 enzyme, and genetic polymorphisms in the human UDP-glucuronosyltransferase-1A7 (UGTIA7) gene were detected.
What does a glucuronide do?
The human body uses glucuronidation to make a large variety of substances more water-soluble, and, in this way, allow for their subsequent elimination from the body through urine or feces (via bile from the liver). Hormones are glucuronidated to allow for easier transport around the body.
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 the UGT in Spain?
The Unión General de Trabajadores (UGT, General Union of Workers) is a major Spanish trade union, historically affiliated with the Spanish Socialist Workers’ Party (PSOE).
What is UGT tank?
Our range of products include RCC Under Ground Water Tank Construction Service.
What does grit mean?
GRIT. Growth Resilience Integrity And Tenacity.
Why is the inhibition of the UGT enzymes important?
The inhibition of the UGT enzymes and its significance Uridine glucuronyl transferases (UGT) are a family of enzymes which play a major role in the Phase II metabolism of drugs. One in ten of the top two hundred prescribed drugs have glucuronidation as a clearance mechanism illustrating the importance of UGTs in drug metabolism.
Are there any clinical studies for UGT inhibition?
The regulatory authorities are now recommending that UGT inhibition is evaluated as part of in vitro drug-drug interaction (DDI) packages to determine if clinical DDI studies are required.
How does UGT inhibition work in Cyprotex ADME?
UGT inhibition is one of Cyprotex’s in vitro experimental ADME services. Cyprotex deliver consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements. Uridine glucuronyl transferases (UGT) are a family of enzymes which play a major role in the Phase II metabolism of drugs.
How is IC 50 determined in UGT inhibition assay?
In Cyprotex’s UGT inhibition assay, a decrease in the formation of the UGT-specific metabolite compared to the vehicle control is used to calculate an IC 50 value (test compound which produces 50% inhibition). Follow-up K i determination is also available if required.