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Xenobiotica
the fate of foreign compounds in biological systems
Volume 39, 2009 - Issue 2
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Research Article

Validation of cytochrome P450 time-dependent inhibition assays: a two-time point IC50 shift approach facilitates kinact assay design

E. S. PerloffBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USACorrespondence[email protected]
,
A. K. MasonBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
S. S. DehalBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
A. P. BlanchardBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
L. MorganBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
T. HoBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
A. DandeneauBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
R. M. CrockerBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
C. M. ChandlerBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
N. BoilyBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
,
C. L. CrespiBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
&
D. M. StresserBD Biosciences Discovery Labware, BD Gentest Contract Research Services, Woburn, MA, USA
 show all
Pages 99-112 | Received 22 Oct 2008, Accepted 20 Nov 2008, Published online: 01 Feb 2009

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Nancy Chen, Donghui Cui, Qing Wang, Zhiming Wen, Richard D. Finkelman & Devin Welty. (2018) In vitro drug–drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica 48:6, pages 637-646.
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Donna A Volpe & Praveen V Balimane. (2018) Application of in vitro CYP and Transporter Assays to Predict Clinical Drug–Drug Interactions. Bioanalysis 10:9, pages 619-623.
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Qiang-Hong Pu, Liang Shi & Chao Yu. (2015) Time-dependent inhibition of CYP3A4 by gallic acid in human liver microsomes and recombinant systems. Xenobiotica 45:3, pages 213-217.
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David M Stresser, Jialin Mao, Jane R Kenny, Barry C Jones & Kenneth Grime. (2014) Exploring concepts of in vitro time-dependent CYP inhibition assays. Expert Opinion on Drug Metabolism & Toxicology 10:2, pages 157-174.
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Noriaki Yoda, Chie Emoto, Shoichi Date, Satoshi Kondo, Masateru Miyake, Satoru Nakazato, Ken Umehara & Eiji Kashiyama. (2012) Characterization of intestinal and hepatic P450 enzymes in cynomolgus monkeys with typical substrates and inhibitors for human P450 enzymes. Xenobiotica 42:8, pages 719-730.
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Rumin Zhang & Frederick Monsma. (2010) Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs. Expert Opinion on Drug Discovery 5:11, pages 1023-1029.
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Howard J. Burt, Aleksandra Galetin & J. Brian Houston. (2010) IC50-based approaches as an alternative method for assessment of time-dependent inhibition of CYP3A4. Xenobiotica 40:5, pages 331-343.
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