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https://www.ncbi.nlm.nih.gov/books/NBK294473/
May 27, 2015 · Irinotecan is a topoisomerase inhibitor that is widely used in the treatment of cancer. It is often used in combination with other drugs to treat metastatic colorectal cancer. However, irinotecan therapy is associated with a high incidence of toxicity, including severe neutropenia and diarrhea (1, 2).Cited by: 5
https://www.ncbi.nlm.nih.gov/pubmed/25033762
Quantitative ADME proteomics - CYP and UGT enzymes in the Beagle dog liver and intestine. Heikkinen AT(1), Friedlein A, Matondo M, Hatley OJ, Petsalo A, Juvonen R, Galetin A, Rostami-Hodjegan A, Aebersold R, Lamerz J, Dunkley T, Cutler P, Parrott N.Cited by: 24
https://www.sciencedirect.com/topics/neuroscience/glucuronosyltransferase
UGT1A1 metabolizes several drugs and endogenous compounds (e.g. bilirubin and estrogen), and is the most extensively studied enzyme of the UGT superfamily. The expression of this enzyme is highly variable, and genetic polymorphisms in the gene contribute to this. Over 30 genetic variants, many of which influence its function, have been reported.
https://www.corning.com/emea/en/products/life-sciences/products/adme-tox-research/recombinant-metabolic-enzymes.html
Recombinant Metabolic Enzymes; ... Support for essential assays, such as reaction phenotyping and enzyme inhibition, required for FDA new drug registration and other pharmacokinetic studies that are appropriate for evaluating pro-drugs with CYP and/or non-CYP pathways of elimination. ... P450, FMOs, OR), and a UDPGA Cofactor System for UGT ...
https://ghr.nlm.nih.gov/gene/UGT1A1
Oct 15, 2019 · Mutations in the UGT1A1 gene that cause Crigler-Najjar syndrome result in reduced or absent function of the bilirubin-UGT enzyme. People with Crigler-Najjar syndrome type 1 (CN1) have no enzyme function, while people with Crigler-Najjar syndrome type 2 …
http://dmd.aspetjournals.org/content/40/5/1051
May 01, 2012 · The measurement of the effect of new chemical entities on human UDP-glucuronosyltransferase (UGT) marker activities using in vitro experimentation represents an important experimental approach in drug development to guide clinical drug-interaction study designs or support claims that no in vivo interaction will occur. Selective high-performance liquid chromatography-tandem …Cited by: 122
https://en.wikipedia.org/wiki/UDP_glucuronosyltransferase_1_family,_polypeptide_A1
UDP-glucuronosyltransferase 1-1 also known as UGT-1A is an enzyme that in humans is encoded by the UGT1A1 gene.. UGT-1A is a uridine diphosphate glucuronosyltransferase (UDP-glucuronosyltransferase, UDPGT), an enzyme of the glucuronidation pathway that transforms small lipophilic molecules, such as steroids, bilirubin, hormones, and drugs, into water-soluble, excretable metabolites.Aliases: UGT1A1, BILIQTL1, GNT1, HUG-BR1, …
https://www.sciencedirect.com/topics/neuroscience/glucuronidation
As listed in Table 24.5, the enzyme catalyzing this reaction consists of a number of proteins coded by genes of the UGT superfamily [25,63–66]. The human UDPGA transferases (UGT) known to metabolize xenobiotics are the products of two gene families, UGT1 and UGT2.
https://www.geneticsdigest.com/the-genetic-basis-of-gilberts-syndrome-an-overview/
Mar 11, 2019 · The most common genetic mutation (permanent alteration in the DNA sequence) that produces Gilbert’s syndrome occurs in an area of DNA near the UGT1A1 gene, known as promoter region, which controls the production of the UGT enzyme. As a result, this genetic mutation impairs the UGT enzyme production.
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