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320 results

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Inhibition of UGT1A1*1 and UGT1A1*6 catalyzed glucuronidation of SN-38 by silybins.
Li W, Chen YN, Chen YY, Wang Z, Wang Z, Jiang LL, Shi HC, Liu Y. Li W, et al. Chem Biol Interact. 2022 Dec 1;368:110248. doi: 10.1016/j.cbi.2022.110248. Epub 2022 Nov 5. Chem Biol Interact. 2022. PMID: 36343684
To evaluate whether SN-38 metabolism can be affected by milk thistle products, the inhibitory effects of silybins on UGT1A1*1 and UGT1A1*6 were evaluated in the present investigation. Both silybin A and silybin B potently inhibited SN-38 glucuronidation catalyzed by …
To evaluate whether SN-38 metabolism can be affected by milk thistle products, the inhibitory effects of silybins on UGT1A1*1 and …
Gene Therapy in Patients with the Crigler-Najjar Syndrome.
D'Antiga L, Beuers U, Ronzitti G, Brunetti-Pierri N, Baumann U, Di Giorgio A, Aronson S, Hubert A, Romano R, Junge N, Bosma P, Bortolussi G, Muro AF, Soumoudronga RF, Veron P, Collaud F, Knuchel-Legendre N, Labrune P, Mingozzi F. D'Antiga L, et al. N Engl J Med. 2023 Aug 17;389(7):620-631. doi: 10.1056/NEJMoa2214084. N Engl J Med. 2023. PMID: 37585628 Clinical Trial.
BACKGROUND: Patients with the Crigler-Najjar syndrome lack the enzyme uridine diphosphoglucuronate glucuronosyltransferase 1A1 (UGT1A1), the absence of which leads to severe unconjugated hyperbilirubinemia that can cause irreversible neurologic injury and death. ...METHODS …
BACKGROUND: Patients with the Crigler-Najjar syndrome lack the enzyme uridine diphosphoglucuronate glucuronosyltransferase 1A1 (UGT1A1 …
Generation of Caco-2 cells stably expressing CYP3A4.POR.UGT1A1 and CYP3A4.POR.UGT1A1*6 using a PITCh system.
Negoro R, Yamada N, Watanabe K, Kono Y, Fujita T. Negoro R, et al. Arch Toxicol. 2022 Feb;96(2):499-510. doi: 10.1007/s00204-021-03175-0. Epub 2021 Oct 16. Arch Toxicol. 2022. PMID: 34654938
The CYP3A4.POR.UGT1A1*6 KI-Caco-2 cells were sensitive to SN-38-induced intestinal toxicity. ...We also developed an intestinal epithelial cell model of patients with UGT1A1*6 and showed that it was useful as a tool for drug discovery....
The CYP3A4.POR.UGT1A1*6 KI-Caco-2 cells were sensitive to SN-38-induced intestinal toxicity. ...We also developed an intest …
High Expression of UGT1A1/1A6 in Monkey Small Intestine: Comparison of Protein Expression Levels of Cytochromes P450, UDP-Glucuronosyltransferases, and Transporters in Small Intestine of Cynomolgus Monkey and Human.
Akazawa T, Uchida Y, Miyauchi E, Tachikawa M, Ohtsuki S, Terasaki T. Akazawa T, et al. Mol Pharm. 2018 Jan 2;15(1):127-140. doi: 10.1021/acs.molpharmaceut.7b00772. Epub 2017 Dec 5. Mol Pharm. 2018. PMID: 29140712
UGT1A1 in jejunum and ileum were >4.57- and >3.11-fold and UGT1A6 in jejunum and ileum were >16.1- and >8.57-fold, respectively, more highly expressed in monkey than in human. ...These findings should be helpful to understand species differences of the function …
UGT1A1 in jejunum and ileum were >4.57- and >3.11-fold and UGT1A6 in jejunum and ileum were >16.1- and >8.57-fold, respec …
Raloxifene glucuronidation in human intestine, kidney, and liver microsomes and in human liver microsomes genotyped for the UGT1A1*28 polymorphism.
Trdan Lusin T, Trontelj J, Mrhar A. Trdan Lusin T, et al. Drug Metab Dispos. 2011 Dec;39(12):2347-54. doi: 10.1124/dmd.111.041897. Epub 2011 Sep 21. Drug Metab Dispos. 2011. PMID: 21937736
Incubation of raloxifene with human liver microsomes genotyped for UGT1A1*28 showed a significantly reduced metabolic clearance toward M1 in microsomes from donors with *28 allele. ...In conclusion, our results show the high importance of the liver and intestine in …
Incubation of raloxifene with human liver microsomes genotyped for UGT1A1*28 showed a significantly reduced metabolic clearance towar …
Association between UGT1A1 gene polymorphism and safety and efficacy of irinotecan monotherapy as the third-line treatment for advanced gastric cancer.
Yamaguchi T, Iwasa S, Shoji H, Honma Y, Takashima A, Kato K, Hamaguchi T, Higuchi K, Boku N. Yamaguchi T, et al. Gastric Cancer. 2019 Jul;22(4):778-784. doi: 10.1007/s10120-018-00917-5. Epub 2019 Jan 2. Gastric Cancer. 2019. PMID: 30603911
METHODS: Efficacy and safety in advanced gastric cancer patients, who were tested for UGT1A1*6 and *28 genotype and treated with irinotecan monotherapy as third-line treatment from 2009 to 2014, were evaluated according to the UGT1A1*6 and *28 genotypes. RESULTS: Am …
METHODS: Efficacy and safety in advanced gastric cancer patients, who were tested for UGT1A1*6 and *28 genotype and treated with irin …
Prediction of Drug-Drug Interaction Between Dabrafenib and Irinotecan via UGT1A1-Mediated Glucuronidation.
Wang Z, Wang X, Wang Z, Fan X, Yan M, Jiang L, Xia Y, Cao J, Liu Y. Wang Z, et al. Eur J Drug Metab Pharmacokinet. 2022 May;47(3):353-361. doi: 10.1007/s13318-021-00740-x. Epub 2022 Feb 11. Eur J Drug Metab Pharmacokinet. 2022. PMID: 35147853
However, the ratios of intra-enterocyte concentration of dabrafenib to K(i,u) ([I](gut)/K(i,u)) are 2.73 and 8.72 in HLMs and recombinant UGT1A1, respectively, indicating a high risk of intestinal DDI when dabrafenib was used in combination with irinotecan. CONCLUSI …
However, the ratios of intra-enterocyte concentration of dabrafenib to K(i,u) ([I](gut)/K(i,u)) are 2.73 and 8.72 in HLMs and recombinant …
Effects of cyclosporin A on the pharmacokinetics and toxicities of irinotecan mediated by UGT1A1 in vitro and in vivo.
Qin Y, Wang N, Chen F, Han X, Zhu Y, Rang Y, Zhai X, Lu Y. Qin Y, et al. Pharmazie. 2020 May 1;75(5):186-190. doi: 10.1691/ph.2020.0316. Pharmazie. 2020. PMID: 32393425
In the liver microsome incubation system, the IC(50) of CsA for UGT1A1 enzyme was 9.4 muM. Furthermore, the UGT1A1 mRNA and protein expression levels were significantly reduced. The present study indicated that CsA treatment could enhance the systemic exposure and t …
In the liver microsome incubation system, the IC(50) of CsA for UGT1A1 enzyme was 9.4 muM. Furthermore, the UGT1A1 mRNA and pr …
Farnesol is glucuronidated in human liver, kidney and intestine in vitro, and is a novel substrate for UGT2B7 and UGT1A1.
Staines AG, Sindelar P, Coughtrie MW, Burchell B. Staines AG, et al. Biochem J. 2004 Dec 15;384(Pt 3):637-45. doi: 10.1042/BJ20040997. Biochem J. 2004. PMID: 15320866 Free PMC article.
Results indicate that farnesol is a good substrate for glucuronidation in human liver, kidney and intestine microsomes (values in nmol/min per mg). Initial analysis using expressed human UGTs indicated that UGTs 1A1 and 2B7 were primarily responsible for glucuronidation in …
Results indicate that farnesol is a good substrate for glucuronidation in human liver, kidney and intestine microsomes (values in nmo …
UGT1A1 and UGT1A3 activity and inhibition in human liver and intestinal microsomes and a recombinant UGT system under similar assay conditions using selective substrates and inhibitors.
Mullapudi TVR, Ravi PR, Thipparapu G. Mullapudi TVR, et al. Xenobiotica. 2021 Nov;51(11):1236-1246. doi: 10.1080/00498254.2021.1998732. Epub 2021 Nov 10. Xenobiotica. 2021. PMID: 34698602
In vitro enzyme kinetics and inhibition data was compared for UGT1A1 and UGT1A3 isoforms under similar assay conditions using human liver microsomes (HLM), human intestinal microsomes (HIM) and recombinant UGT (rUGT) enzyme systems.UGT1A1 catalysed beta-estra …
In vitro enzyme kinetics and inhibition data was compared for UGT1A1 and UGT1A3 isoforms under similar assay conditions using human l …
320 results