HLM chip – A microfluidic approach to study the mechanistic basis of cytochrome P450 inhibition using immobilized human liver microsomes

Author:

Pihlaja Tea,Kiiski Iiro,Sikanen TiinaORCID

Funder

Research Council of Finland

Strategic Research Council

Publisher

Elsevier BV

Reference47 articles.

1. An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes;Berry;Drug Metab. Lett.,2008

2. The conduct of in vitro and in vivo drug-drug interaction studies: a pharmaceutical research and manufacturers of America (PhRMA) perspective;Bjornsson;Drug Metab. Dispos.,2003

3. Use of isolated hepatocyte preparations for cytochrome P450 inhibition studies: comparison with microsomes for Ki determination;Brown;Drug Metab. Dispos.,2007

4. Pitfalls in the design of metabolism-dependent CYP inhibition (MDI) experiments with a dilution step: inhibitor depletion by metabolism and/or microsomal binding leads to underestimation of the shifted IC50 value;Buckley;Drug Metab. Rev.,2010

5. Stoichiometry and physical chemistry of promiscuous aggregate-based inhibitors;Coan;J. Am. Chem. Soc.,2008

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