β-Lactam analogues of combretastatin A-4 prevent metabolic inactivation by glucuronidation in chemoresistant HT-29 colon cancer cells.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.02.049
Abstract: Glucuronidation by uridine 5-diphosphoglucuronosyl transferase enzymes (UGTs) is a cause of intrinsic drug resistance in cancer cells. Glucuronidation of combretastatin A-4 (CA-4) was previously identified as a mechanism of resistance in hepatocellular cancer cells. Herein,… read more here.
Keywords: glucuronidation; resistance; colon cancer; cancer cells ... See more keywords
GLI1-Inducible Glucuronidation Targets a Broad Spectrum of Drugs.
Sign Up to like & getrecommendations! Published in 2019 at "ACS chemical biology"
DOI: 10.1021/acschembio.8b01118
Abstract: Cancer therapies are plagued by resistance. Previously, we discovered a novel form of cancer drug resistance where the Glioma-associated protein 1 (GLI1) elevates UGT1A glucuronidation enzymes, thereby glucuronidating cytarabine and ribavirin, leading to resistance in… read more here.
Keywords: gli1 inducible; glucuronidation; inducible glucuronidation; resistance ... See more keywords
Identification of UGTs and BCRP as potential pharmacokinetic determinants of the natural flavonoid alpinetin
Sign Up to like & getrecommendations! Published in 2019 at "Xenobiotica"
DOI: 10.1080/00498254.2018.1440657
Abstract: Abstract Alpinetin is a natural flavonoid showing a variety of pharmacological effects such as anti-inflammatory, anti-tumor and hypolipidemic activities. Here, we aim to determine the roles of UDP-glucuronosyltransferases (UGTs) and breast cancer resistance protein (BCRP)… read more here.
Keywords: glucuronidation; min nmol; alpinetin; activity ... See more keywords
Enzymatic analysis of glucuronidation of synthetic cannabinoid 1-naphthyl 1-(4-fluorobenzyl)-1H-indole-3-carboxylate (FDU-PB-22)
Sign Up to like & getrecommendations! Published in 2019 at "Xenobiotica"
DOI: 10.1080/00498254.2019.1580403
Abstract: Abstract Recently, there has been a rise in abuse of synthetic cannabinoids (SCBs). The consumption of SCBs results in various effects and can induce toxic reactions, including paranoia, seizures, tachycardia and even death. 1-Naphthyl 1-(4-fluorobenzyl)-1H-indole-3-carboxylate… read more here.
Keywords: fluorobenzyl indole; glucuronidation; fdu; indole carboxylate ... See more keywords
Uridine diphosphate glucuronosyltransferase 1A1
Sign Up to like & getrecommendations! Published in 2019 at "Xenobiotica"
DOI: 10.1080/00498254.2019.1617910
Abstract: Abstract The role that the phase-II reaction, glucuronidation, plays in the biotransformation of endo and xenobiotics is discussed with particular emphasis given to the UGT1A1 isoenzyme. This individual isoenzyme is responsible for both the mono… read more here.
Keywords: irinotecan belinostat; uridine diphosphate; glucuronidation; glucuronosyltransferase 1a1 ... See more keywords
Effects of common genetic variants of human uridine diphosphate glucuronosyltransferase subfamilies on irinotecan glucuronidation
Sign Up to like & getrecommendations! Published in 2022 at "Toxicology Mechanisms and Methods"
DOI: 10.1080/15376516.2022.2109229
Abstract: Abstract The adverse effects (diarrhea and neutropenia) of irinotecan (7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin) are associated with genetic variants of uridine diphosphate glucuronosyltransferase 1A subfamilies (UGT1As). UGT1As are enzymes that metabolize the active form of irinotecan, 7-ethyl-10 hydroxycamptothecin (SN-38),… read more here.
Keywords: genetic variants; adverse effects; glucuronidation; glucuronosyltransferase subfamilies ... See more keywords
Drug and Chemical Glucosidation by Control Supersomes and Membranes from Spodoptera frugiperda (Sf) 9 Cells: Implications for the Apparent Glucuronidation of Xenobiotics by UDP-glucuronosyltransferase 1A5
Sign Up to like & getrecommendations! Published in 2018 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.118.084947
Abstract: Accumulating evidence indicates that several human UDP-glucuronosyltransferase (UGT) enzymes catalyze both glucuronidation and glucosidation reactions. Baculovirus-infected insect cells [Trichoplusia ni and Spodoptera frugiperda (Sf9)] are used widely for the expression of recombinant human UGT enzymes.… read more here.
Keywords: udp glucuronosyltransferase; glucosidation; glucuronidation; control ... See more keywords
Role of l- and d-Menthol in the Glucuronidation and Detoxification of the Major Lung Carcinogen, NNAL
Sign Up to like & getrecommendations! Published in 2019 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.119.088351
Abstract: Menthol, which creates mint flavor and scent, is often added to tobacco in both menthol and nonmenthol cigarettes. A potent tobacco carcinogen, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK), is extensively metabolized to its equally carcinogenic metabolite 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL) as… read more here.
Keywords: tobacco; glucuronidation; nnal gluc; carcinogen ... See more keywords
Circadian Clock Component Rev-erbα Regulates Diurnal Rhythm of UDP-Glucuronosyltransferase 1a9 and Drug Glucuronidation in Mice
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.120.000030
Abstract: UDP-glucuronosyltransferases (UGTs) are a family of phase II enzymes that play an important role in metabolism and elimination of numerous endo- and xenobiotics. Here, we aimed to characterize diurnal rhythm of Ugt1a9 in mouse liver… read more here.
Keywords: erb; metabolism; glucuronidation; circadian clock ... See more keywords
Characterization of Enzymes Involved in Nintedanib Metabolism in Humans
Sign Up to like & getrecommendations! Published in 2023 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.122.001113
Abstract: Nintedanib, which is used to treat idiopathic pulmonary fibrosis and non–small cell lung cancer, is metabolized to a pharmacologically inactive carboxylate derivative, BIBF1202, via hydrolysis and subsequently by glucuronidation to BIBF1202 acyl-glucuronide (BIBF1202-G). Since BIBF1202-G… read more here.
Keywords: glucuronidation; min per; nintedanib metabolism; bibf1202 ... See more keywords
Effects of a novel UGT2B haplotype and UGT1A4*3 allele variants on glucuronidation of clozapine in vivo.
Sign Up to like & getrecommendations! Published in 2022 at "Current drug metabolism"
DOI: 10.2174/1389200223666220201152953
Abstract: BACKGROUND Glucuronidation is an important metabolic pathway of clozapine (CLZ), but the impact of various uridine 5'diphospho-glucuronosyltransferases (UGT) polymorphisms on the exposure and metabolism of CLZ in vivo is unclear. OBJECTIVE The objective of this… read more here.
Keywords: exposure; haplotype ugt1a4; clz; glucuronidation ... See more keywords