Cytochrome P450 inhibition assay

Di, L. et al. 2006. Comparison of cytochrome P450 inhibition assays for drug discovery using human liver microsomes with LC-MS, rhCYP450 isozymes with fluorescence, and double cocktail with LC/ S. Int. J. Pharmaceut. http //dx.doi.org/10.1016/j.ijpharm.2006.10.039. 

D. M. High-throughput cytochrome p450 inhibition assays by ultrafast gradient liquid chromatography with tandem mass spectrometry using monolithic columns. Rapid Commun Mass Spectrom 2003, 17, 509-518. 

S.X. Peng, A.G. Barbone, D.M. Ritchie, High-throughput cytochrome P450 inhibition assays by ultrafast gradient LC-MS-MS using monolithic columns. Rapid Commun. Mass Spectrom., 17 (2003) 509. 

Wu, J. et al., High-throughput cytochrome P450 inhibition assays using laser diode thermal desorption-atmospheric pressure chemical ionization-tandem mass spectrometry, Anal. Chem., 79, 4657, 2007. 

Biological/Medical Applications As a substrate for measuring cytochrome P 450 enzymes activity cytochrome P450 inhibition assays drug design - drug metabolism " treating viral or parasite infections " ... 

Miller, V. R Stresser, D. Crespi, C. L. The use of fluorescein aryl ethers in high throughput cytochrome P450 inhibition assays. PCX Int. Appl. WO 2001014361, 2001. 

Jenkins, K.M. et al. 2004. Automated high throughput ADME assays for metabolic stability and cytochrome P450 inhibition profiling of combinatorial libraries. J. Pharm. Biomed. Anal. 34 989. 

Naritomi, Y. et al. Utility of microtiter plate assays for human cytochrome P450 inhibition studies in drug discovery. Drug Metab. Pharmacokin. 19 55. 

The following discussions and assay descriptions are related to cytochrome P450 inhibition. Most drug interaction studies are related to P450 isoenzymes. Nevertheless, other enzyme systems may contribute to significant drug interactions such as transporter (e.g. Floren 1997 Abel 2001) phase II enzymes (e.g. Diet-mann 1976 Zucker 2001 Rayer 2001 Williams 2004), or cytosolic enzymes (Obach 2004). Additional assays related to pgp, phase II or cytosolic enzyme interactions are published in literature (e.g. Polli 2001 Schwab 2002 Schinkel 2003 www.bdbiosciences.com, Obach 2004). 

Wu X, Wang J, Tan L et al (2012) In vitro ADME profiling using high-throughput rapid-fire mass spectrometry cytochrome p450 inhibition and metabolic stability assays. J Biomol Screen 17 761-772... 

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