Cytochrome P450 Induction

LeCluyse, Edward L.; Sinz, Michael; Hewitt, Nicola J.; Ferguson, Stephen S. G.; Sahi, Jasminder

doi:10.1002/9780470538951.ch8

Cited by 4 publications

(2 citation statements)

References 104 publications

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“…In this regard, Hc3716-hTERT immortalized hepatocytes constitute an appropriate in vitro model for predicting the side-effects of telomere-targeting drugs (39). Furthermore, Fa2N4 cells may be used as a routine screening system for pregnane X receptor-mediated CYP3A4 induction (92). Similarly, the hepatic THLE cell line and THLE-CYP sublines have been reported as promising models for investigation of CYP-mediated drug metabolism and liver toxicity (63, 93-95).…”

Section: In Vitro Applications Of Immortalized Human Hepatocytesmentioning

confidence: 99%

Immortalized Human Hepatic Cell Lines for In Vitro Testing and Research Purposes

Ramboer

Vanhaecke

Rogiers

et al. 2014

Methods in Molecular Biology

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SummaryThe ubiquitous shortage of primary human hepatocytes has urged the scientific community to search for alternative cell sources, such as immortalized hepatic cell lines. Over the years, several human hepatic cell lines have been produced, whether or not using a combination of viral oncogenes and human telomerase reverse transcriptase protein. Conditional approaches for hepatocyte immortalization have also been established and allow generation of growth-controlled cell lines. A variety of immortalized human hepatocytes have already proven useful as tools for liver-based in vitro testing and fundamental research purposes. The present chapter describes currently applied immortalization strategies and provides an overview of the actually available immortalized human hepatic cell lines and their in vitro applications.

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Section: In Vitro Applications Of Immortalized Human Hepatocytesmentioning

confidence: 99%

Immortalized Human Hepatic Cell Lines for In Vitro Testing and Research Purposes

Ramboer

Vanhaecke

Rogiers

et al. 2014

Methods in Molecular Biology

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show abstract

“…In silico modeling of CYP induction is very challenging due to the requirement of availability of crystal structure of nuclear receptors along with well-understood structural biology [75]. In addition, due to large binding pocket of some of the receptors, especially PXR, combined with the ability of the ligands to bind to several regions of the nuclear receptors further complicates modeling.…”

Section: In Silicomentioning

confidence: 99%

ADMEProfiling in Drug Discovery and Development: An Overview

Bohnert

Prakash

2012

Encyclopedia of Drug Metabolism and Interactions

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The applications of parallel synthesis and combinatory chemistry to expedite lead finding and lead optimization processes have shifted the chemical libraries toward poorer biopharmaceutical, ADME (absorption, distribution, metabolism, and excretion), and pharmacokinetic (PK) properties. A drug candidate should have desirable biopharmaceutical properties such as good solubility and good permeability, as well as optimal and ADME/PK properties. The early knowledge of liability of biopharmaceutical, ADME/PK, and DDI properties is very valuable in drug candidate selection process. In the last one decade, multiple in silico, in vitro, and in vivo ADME studies have been developed and implemented in the drug discovery and development process to alert chemists and drug metabolism scientists of the potential ADME, PK and DDI issues in the clinic. In this chapter, we attempt to discuss these various ADME profiling approaches in drug discovery and development process and the latest technologies of the selected assays.

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In Vitro Experimental Models for Studying Drug Biotransformation

Bohnert

Gan

2013

Handbook of Metabolic Pathways of Xenobiotics

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Cytochrome P450 Induction

Cited by 4 publications

References 104 publications

Immortalized Human Hepatic Cell Lines for In Vitro Testing and Research Purposes

Immortalized Human Hepatic Cell Lines for In Vitro Testing and Research Purposes

ADMEProfiling in Drug Discovery and Development: An Overview

In Vitro Experimental Models for Studying Drug Biotransformation

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