Pharmacokinetic drug interactions involving 17α-ethinylestradiol: a new look at an old drug

…, B Wang, YH Han, P Balimane, Z Yang, M Sinz… - Clinical …, 2007 - Springer
… and 2A1) was characterised by relatively high K m values (K m >230 nmol/L). A more … a
two-K m process with low and high K m components. The low K m component of EE sulfation was …

[HTML][HTML] Current industrial practices in assessing CYP450 enzyme induction: preclinical and clinical

M Sinz, G Wallace, J Sahi - The AAPS journal, 2008 - Springer
Induction of drug metabolizing enzymes, such as the cytochromes P450 (CYP) is known to
cause drug-drug interactions due to increased elimination of co-administered drugs. This …

Cytochrome P450 reaction-phenotyping: an industrial perspective

H Zhang, CD Davis, MW Sinz… - Expert opinion on drug …, 2007 - Taylor & Francis
… Integration of the data is key because it is the product of f m and f m,CYP (ie, f m × f m,CYP
) that governs the magnitude of a drug interaction, and the impact of a CYP polymorphism on …

CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes

…, M Cunningham, S Kim, T Burn, J Lin, M Sinz… - Drug Metabolism and …, 2002 - ASPET
Induction of cytochrome P450 3A4 (CYP3A4) is determined typically by employing primary
culture of human hepatocytes and measuring CYP3A4 mRNA, protein and microsomal activity…

Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice

K He, KR Iyer, RN Hayes, MW Sinz… - Chemical research in …, 1998 - ACS Publications
… The indicated sites of oxidation are based on the CID behavior of the precursor ion of m/z
355; viz., the product ion of m/z 203 corresponds to the intact 5-hydroxypsoralen moiety, and …

Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole

H Huang, H Wang, M Sinz, M Zoeckler, J Staudinger… - Oncogene, 2007 - nature.com
Individual variation in drug metabolism is a major cause of unpredictable side effects during
therapy. Drug metabolism is controlled by a class of orphan nuclear receptors (NRs), which …

Preclinical profile and characterization of the hepatitis C virus NS3 protease inhibitor asunaprevir (BMS-650032)

…, MS Lee, K Mosure, LQ Sun, M Sinz… - Antimicrobial agents …, 2012 - Am Soc Microbiol
… Analysis of the data revealed that as concentrations increased, the apparent K m for the
substrate increased while the maximal enzyme turnover rate (V max ) remained constant, typical …

Human pregnane X receptor antagonists and agonists define molecular requirements for different binding sites

…, M Iyer, V Kholodovych, N Ai, WJ Welsh, M Sinz… - Molecular …, 2007 - ASPET
The pregnane X receptor (PXR) is an important transcriptional regulator of the expression of
xenobiotic metabolism and transporter genes. The receptor is promiscuous, binding many …

In vitro and in vivo induction of cytochrome p450: a survey of the current practices and recommendations: a pharmaceutical research and manufacturers of america …

…, D Moore, S Ripp, J Silva, V Sinha, M Sinz… - Drug Metabolism and …, 2009 - ASPET
… We thank M. Garvin and the PhRMA team for compiling the anonymous survey responses.
We also gratefully acknowledge input from the PhRMA Drug Metabolism Technical Group …

Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers

…, M Zoeckler, R Schartman, M Sinz… - Proceedings of the …, 2011 - National Acad Sciences
Influenza nucleoprotein (NP) plays multiple roles in the virus life cycle, including an essential
function in viral replication as an integral component of the ribonucleoprotein complex, …