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Role of vitamin D receptor in the regulation of CYP3A gene expression.
Qin X, Wang X. Qin X, et al. Acta Pharm Sin B. 2019 Nov;9(6):1087-1098. doi: 10.1016/j.apsb.2019.03.005. Epub 2019 Apr 4. Acta Pharm Sin B. 2019. PMID: 31867158 Free PMC article. Review.
VD(3) is converted to the active form, 1α,25-dihydroxyvitamin D(3) (1,25-D3), by cytochrome P450 2R1 (CYP2R1)/CYP27A1 and CYP27B1 sequentially, and deactivated by multiple enzymes including CYP3A4. ...In rats, intestinal Cyp3a1 and Cyp3a2 mRNAs were induced by 1,25- …
VD(3) is converted to the active form, 1α,25-dihydroxyvitamin D(3) (1,25-D3), by cytochrome P450 2R1 (CYP2R1)/CYP27A1 and CYP27B1 seq …
Ligand diversity of human and chimpanzee CYP3A4: activation of human CYP3A4 by lithocholic acid results from positive selection.
Kumar S, Qiu H, Oezguen N, Herlyn H, Halpert JR, Wojnowski L. Kumar S, et al. Drug Metab Dispos. 2009 Jun;37(6):1328-33. doi: 10.1124/dmd.108.024372. Epub 2009 Mar 19. Drug Metab Dispos. 2009. PMID: 19299527 Free PMC article.
A striking exception was the hepatotoxic secondary bile acid lithocholic acid, which at saturation caused a 5-fold increase in 7-BFC debenzylation by human CYP3A4 but not by chimpanzee CYP3A4. Mutagenesis of human CYP3A4 revealed that at …
A striking exception was the hepatotoxic secondary bile acid lithocholic acid, which at saturation caused a 5-fold incr …
Angiopoietin-Like Protein 8 Is a Novel Vitamin D Receptor Target Gene Involved in Nonalcoholic Fatty Liver Pathogenesis.
García-Monzón C, Petrov PD, Rey E, Marañón P, Del Pozo-Maroto E, Guzmán C, Rodríguez de Cía J, Casado-Collado AJ, Vargas-Castrillón J, Saez A, Miquilena-Colina ME, Lo Iacono O, Castell JV, González-Rodríguez Á, Jover R. García-Monzón C, et al. Am J Pathol. 2018 Dec;188(12):2800-2810. doi: 10.1016/j.ajpath.2018.07.028. Epub 2018 Sep 22. Am J Pathol. 2018. PMID: 30248338 Free article.
The mRNA levels of hepatic VDR- and vitamin D-related genes [cytochrome P450 (CYP) 2R1, CYP27A1, and CYP3A4] were higher in NAFL patients compared with normal liver subjects. ...Moreover, increases in serum conjugated bile acids, including the VDR agonist glycine- …
The mRNA levels of hepatic VDR- and vitamin D-related genes [cytochrome P450 (CYP) 2R1, CYP27A1, and CYP3A4] were higher in NA …
The influences of cholecystectomy on the circadian rhythms of bile acids as well as the enterohepatic transporters and enzymes systems in mice.
Zhang F, Duan Y, Xi L, Wei M, Shi A, Zhou Y, Wei Y, Wu X. Zhang F, et al. Chronobiol Int. 2018 May;35(5):673-690. doi: 10.1080/07420528.2018.1426596. Epub 2018 Jan 30. Chronobiol Int. 2018. PMID: 29381405
ABBREVIATIONS: Asbt: apical sodium-dependent bile acids transporter; AUC24h: area under the 24-hour BA concentration time curve; BAs: bile acids; Bsep: bile salt export pump; β-MCA: β-muricholic acid; CA: cholic acid; CDCA: chenodeoxycholic acid; Cyp3a11: …
ABBREVIATIONS: Asbt: apical sodium-dependent bile acids transporter; AUC24h: area under the 24-hour BA concentration time curve; BAs: bile a …
Regioselective Versatility of Monooxygenase Reactions Catalyzed by CYP2B6 and CYP3A4: Examples with Single Substrates.
Erratico CA, Deo AK, Bandiera SM. Erratico CA, et al. Adv Exp Med Biol. 2015;851:131-49. doi: 10.1007/978-3-319-16009-2_5. Adv Exp Med Biol. 2015. PMID: 26002734 Review.
Hepatic microsomal cytochrome P450 (CYP) enzymes have broad and overlapping substrate specificity and catalyze a variety of monooxygenase reactions, including aliphatic and aromatic hydroxylations, N-hydroxylations, oxygenations of heteroatoms (N, S, P and I), alken …
Hepatic microsomal cytochrome P450 (CYP) enzymes have broad and overlapping substrate specificity and catalyze a variety of monooxyge …
6alpha-hydroxylation of taurochenodeoxycholic acid and lithocholic acid by CYP3A4 in human liver microsomes.
Araya Z, Wikvall K. Araya Z, et al. Biochim Biophys Acta. 1999 Apr 19;1438(1):47-54. doi: 10.1016/s1388-1981(99)00031-1. Biochim Biophys Acta. 1999. PMID: 10216279
Fourteen recombinant expressed cytochrome P450 (CYP) enzymes, human liver microsomes from different donors, and selective cytochrome P450 inhibitors were used to study the hydroxylation of taurochenodeoxycholic acid and lithocholic acid. ...From …
Fourteen recombinant expressed cytochrome P450 (CYP) enzymes, human liver microsomes from different donors, and selective cytochro
Vitamin E analogues differentially inhibit human cytochrome P450 3A (CYP3A)-mediated oxidative metabolism of lithocholic acid: Impact of δ-tocotrienol on lithocholic acid cytotoxicity.
Wong SY, Teo JSM, Chai SF, Yeap SL, Lau AJ. Wong SY, et al. Toxicology. 2019 Jul 1;423:62-74. doi: 10.1016/j.tox.2019.05.005. Epub 2019 May 15. Toxicology. 2019. PMID: 31102695
Lithocholic acid is a cytotoxic bile acid oxidized at the C-3 position by human cytochrome P450 3A (CYP3A) to form 3-ketocholanoic acid, but it is not known whether this metabolite is cytotoxic. ...In the present study, the hypothesis to
Lithocholic acid is a cytotoxic bile acid oxidized at the C-3 position by human cytochrome P450 3A (CYP3A
Rapid and drastic induction of CYP3A4 mRNA expression via vitamin D receptor in human intestinal LS180 cells.
Fukumori S, Murata T, Taguchi M, Hashimoto Y. Fukumori S, et al. Drug Metab Pharmacokinet. 2007 Oct;22(5):377-81. doi: 10.2133/dmpk.22.377. Drug Metab Pharmacokinet. 2007. PMID: 17965521 Free article.
The ability of CYP3A4 mRNA induction in LS180 cells was highly dependent on the site and number of vitamin D(3) and D(2) hydroxylation. In addition, short-time (6 h) treatment of LS180 cells with cytotoxic secondary bile acids, lithocholic acid (LCA) and 3-ke …
The ability of CYP3A4 mRNA induction in LS180 cells was highly dependent on the site and number of vitamin D(3) and D(2) hydroxylatio …
3-ketocholanoic acid is the major in vitro human hepatic microsomal metabolite of lithocholic acid.
Deo AK, Bandiera SM. Deo AK, et al. Drug Metab Dispos. 2009 Sep;37(9):1938-47. doi: 10.1124/dmd.109.027763. Epub 2009 Jun 1. Drug Metab Dispos. 2009. PMID: 19487251
Incubation of lithocholic acid with a of human recombinant P450 enzymes revealed that all five metabolites were formed by recombinant CYP3A4. Chemical inhibition studies with human liver microsomes and recombinant P450 enzymes confirmed that CYP3A4 was …
Incubation of lithocholic acid with a of human recombinant P450 enzymes revealed that all five metabolites were formed by reco …
Microbial-derived lithocholic acid and vitamin K2 drive the metabolic maturation of pluripotent stem cells-derived and fetal hepatocytes.
Avior Y, Levy G, Zimerman M, Kitsberg D, Schwartz R, Sadeh R, Moussaieff A, Cohen M, Itskovitz-Eldor J, Nahmias Y. Avior Y, et al. Hepatology. 2015 Jul;62(1):265-78. doi: 10.1002/hep.27803. Epub 2015 Apr 22. Hepatology. 2015. PMID: 25808545
The liver is the main organ responsible for the modification, clearance, and transformational toxicity of most xenobiotics owing to its abundance in cytochrome P450 (CYP450) enzymes. ...We show that vitamin K2 and lithocholic acid, a by-product of intestinal …
The liver is the main organ responsible for the modification, clearance, and transformational toxicity of most xenobiotics owing to its abun …
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