Importance of target-mediated drug disposition for small molecules

DA Smith, RA Van Waterschoot, NJ Parrott… - Drug discovery today, 2018 - Elsevier
Highlights • Target-mediated drug disposition for small molecules is not addressed systematically.
• TMDD has a major influence on drug distribution and clearance. • TMDD results in …

Molecular modeling-guided site-directed mutagenesis of cytochrome P450 2D6

…, RA B van Waterschoot… - Current drug …, 2007 - ingentaconnect.com
Cytochrome P450 (CYP) 2D6 is one of the most important drug metabolizing enzymes and
the rationalization and prediction of potential CYP2D6 substrates is therefore advantageous …

A critical analysis of the interplay between cytochrome P450 3A and P-glycoprotein: recent insights from knockout and transgenic mice

RAB van Waterschoot, AH Schinkel - Pharmacological reviews, 2011 - ASPET
CYP3A is one of the most important drug-metabolizing enzymes, determining the first-pass
metabolism, oral bioavailability, and elimination of many drugs. It is also an important …

How important is intestinal cytochrome P450 3A metabolism?

AE van Herwaarden, RAB van Waterschoot… - Trends in …, 2009 - cell.com
Cytochrome P450 3A (CYP3A) enzymes metabolize a wide variety of xenobiotics including
many drugs. Because CYP3A is localized in both the liver and intestine, it can make a major …

Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation

JS Lagas, RAB van Waterschoot, RW Sparidans… - Molecular cancer …, 2010 - AACR
… Robert AB van Waterschoot; Robert AB van Waterschoot … We thank Evita van de Steeg
and Dilek Iusuf for critical reading of the manuscript. …

Absence of Both Cytochrome P450 3A and P-glycoprotein Dramatically Increases Docetaxel Oral Bioavailability and Risk of Intestinal Toxicity

RAB van Waterschoot, JS Lagas, E Wagenaar… - Cancer research, 2009 - AACR
Docetaxel is one of the most widely used anticancer drugs. A major problem with docetaxel
treatment, however, is the considerable interpatient variability in docetaxel exposure. …

Inhibition and stimulation of intestinal and hepatic CYP3A activity: studies in humanized CYP3A4 transgenic mice using triazolam

RAB van Waterschoot, RW Rooswinkel… - Drug metabolism and …, 2009 - ASPET
CYP3A4 is an important determinant of drug-drug interactions. In this study, we evaluated
whether cytochrome P450 3A knockout mice [Cyp3a(−/−)] and CYP3A4 transgenic (CYP3A4-…

Brain accumulation of dasatinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by elacridar treatment

JS Lagas, RAB van Waterschoot, VACJ van Tilburg… - Clinical Cancer …, 2009 - AACR
… Robert AB van Waterschoot; Robert AB van Waterschoot … We thank Evita van de Steeg
and Marijn Vlaming for critical reading of the manuscript. …

Midazolam metabolism in cytochrome P450 3A knockout mice can be attributed to up-regulated CYP2C enzymes

RAB van Waterschoot, AE van Herwaarden… - Molecular …, 2008 - ASPET
The cytochrome P450 3A (CYP3A) enzymes represent one of the most important drug-metabolizing
systems in humans. Recently, our group has generated cytochrome P450 3A …

[HTML][HTML] MYRiAD: a multi-array room acoustic database

…, R Ali, M Taseska, T van Waterschoot - EURASIP Journal on …, 2023 - Springer
In the development of acoustic signal processing algorithms, their evaluation in various
acoustic environments is of utmost importance. In order to advance evaluation in realistic and …