Search Results - "GILISSEN, Ron A"

Prediction of Human Pharmacokinetics Using Physiologically Based Modeling: A Retrospective Analysis of 26 Clinically Tested Drugs by DE BUCK, Stefan S, SINHA, Vikash K, FENU, Luca A, NIJSEN, Marjoleen J, MACKIE, Claire E, GILISSEN, Ron A. H. J

“…The aim of this study was to evaluate different physiologically based modeling strategies for the prediction of human pharmacokinetics. Plasma profiles after…”
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The Prediction of Drug Metabolism, Tissue Distribution, and Bioavailability of 50 Structurally Diverse Compounds in Rat Using Mechanism-Based Absorption, Distribution, and Metabolism Prediction Tools by DE BUCK, Stefan S, SINHA, Vikash K, FENU, Luca A, GILISSEN, Ron A, MACKIE, Claire E, NIJSEN, Marjoleen J

“…The aim of this study was to assess a physiologically based modeling approach for predicting drug metabolism, tissue distribution, and bioavailability in rat…”
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Fragment-Based Discovery of Type I Inhibitors of Maternal Embryonic Leucine Zipper Kinase by Johnson, Christopher N, Berdini, Valerio, Beke, Lijs, Bonnet, Pascal, Brehmer, Dirk, Coyle, Joseph E, Day, Phillip J, Frederickson, Martyn, Freyne, Eddy J. E, Gilissen, Ron A. H. J, Hamlett, Christopher C. F, Howard, Steven, Meerpoel, Lieven, McMenamin, Rachel, Patel, Sahil, Rees, David C, Sharff, Andrew, Sommen, François, Wu, Tongfei, Linders, Joannes T. M

“…Fragment-based drug design was successfully applied to maternal embryonic leucine zipper kinase (MELK). A low affinity (160 μM) fragment hit was identified,…”
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Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase by Johnson, Christopher N, Adelinet, Christophe, Berdini, Valerio, Beke, Lijs, Bonnet, Pascal, Brehmer, Dirk, Calo, Frederick, Coyle, Joseph E, Day, Phillip J, Frederickson, Martyn, Freyne, Eddy J. E, Gilissen, Ron A. H. J, Hamlett, Christopher C. F, Howard, Steven, Meerpoel, Lieven, Mevellec, Laurence, McMenamin, Rachel, Pasquier, Elisabeth, Patel, Sahil, Rees, David C, Linders, Joannes T. M

“…A novel Type II kinase inhibitor chemotype has been identified for maternal embryonic leucine zipper kinase (MELK) using structure-based ligand design. The…”
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Predicting Oral Clearance in Humans: How Close Can We Get with Allometry? by Sinha, Vikash K., De Buck, Stefan S., Fenu, Luca A., Smit, Johan W., Nijsen, Marjoleen, Gilissen, Ron A. H. J., Van Peer, Achiel, Lavrijsen, Karel, Mackie, Claire E.

“…Background Oral clearance (CL/F) is an important pharmacokinetic parameter and plays an important role in the selection of a safe and tolerable dose for…”
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Towards a Better Prediction of Peak Concentration, Volume of Distribution and Half-Life after Oral Drug Administration in Man, Using Allometry by Sinha, Vikash K., Vaarties, Karin, De Buck, Stefan S., Fenu, Luca. A., Nijsen, Marjoleen, Gilissen, Ron A. H. J., Sanderson, Wendy, Uytsel, Kelly Van, Hoeben, Eva, Peer, Achiel Van, Mackie, Claire E., Smit, Johan W.

“…Background: It is imperative that new drugs demonstrate adequate pharmacokinetic properties, allowing an optimal safety margin and convenient dosing regimens…”
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Chiral capillary electrophoretic analysis of verapamil metabolism by cytochrome P450 3A4 by Ha, Pham Thi Thanh, Sluyts, Inge, Dyck, Sigrid Van, Zhang, Jie, Gilissen, Ron A.H.J., Hoogmartens, Jos, Schepdael, Ann Van

“…Cytochrome P450 (CYP), which is one of the most important enzymes in human liver, is responsible for a large portion of the first-pass metabolism of drugs…”
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Discovery of Potent, Orally Bioavailable Small-Molecule Inhibitors of the Human CCR2 Receptor by Doyon, Julien, Coesemans, Erwin, Boeckx, Staf, Buntinx, Mieke, Hermans, Bart, Van Wauwe, Jean P., Gilissen, Ron A. H. J., De Groot, Alex H. J., Corens, David, Van Lommen, Guy

“…We recently reported the discovery of a series of 2‐thioimidazoles as CCR2 antagonists. The most potent molecules of this series, the 4,5‐diesters, were…”
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Cardio-vascular safety beyond hERG: in silico modelling of a guinea pig right atrium assay by Fenu, Luca A., Teisman, Ard, De Buck, Stefan S., Sinha, Vikash K., Gilissen, Ron A. H. J., Nijsen, Marjoleen J. M. A., Mackie, Claire E., Sanderson, Wendy E.

“…As chemists can easily produce large numbers of new potential drug candidates, there is growing demand for high capacity models that can help in driving the…”
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Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients by de Witte, Wilhelmus E A, Wong, Yin Cheong, Nederpelt, Indira, Heitman, Laura H, Danhof, Meindert, van der Graaf, Piet H, Gilissen, Ron A H J, de Lange, Elizabeth C M

“…Drug-target binding kinetics are major determinants of the time course of drug action for several drugs, as clearly described for the irreversible binders…”
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Simultaneous measurement of drug metabolic stability and identification of metabolites using ion-trap mass spectrometry by Kantharaj, E., Tuytelaars, An, Proost, Pascale E. A., Ongel, Zuleyha, van Assouw, Harrie P., Gilissen, Ron A. H. J.

“…The use of in vitro drug metabolism data in the understanding of in vivo pharmacokinetic, safety and toxicity data has become a large area of scientific…”
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HERG mutation predicts short QT based on channel kinetics but causes long QT by heterotetrameric trafficking deficiency by PAULUSSEN, Aimée D. C, RAES, Adam, JONGBLOED, Roselie J, GILISSEN, Ron A. H. J, WILDE, Arthur A. M, SNYDERS, Dirk J, SMEETS, Hubert J. M, AERSSENS, Jeroen

“…Mutations in the KCNH2 (hERG, human ether-à-go-go related gene) gene may cause a reduction of the delayed rectifier current I(Kr), thereby leading to the long…”
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Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2 by Buntinx, Mieke, Hermans, Bart, Goossens, Jan, Moechars, Dieder, Gilissen, Ron A H J, Doyon, Julien, Boeckx, Staf, Coesemans, Erwin, Van Lommen, Guy, Van Wauwe, Jean P

“…The interaction between CC chemokine receptor 2 (CCR2) with monocyte chemoattractant proteins, such as MCP-1, regulates the activation and recruitment of…”
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Simultaneous measurement of metabolic stability and metabolite identification of 7-methoxymethylthiazolo[3,2-a]pyrimidin-5-one derivatives in human liver microsomes using liquid chromatography/ion-trap mass spectrometry by Kantharaj, E., Ehmer, Peter B., Tuytelaars, An, Vlaslaer, Anne Van, Mackie, Claire, Gilissen, Ron A. H. J.

“…A liquid chromatography/mass spectrometry (LC/MS) method using an atmospheric pressure chemical ionisation source was used to measure the metabolic stability…”
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The use of liquid chromatography-atmospheric pressure chemical ionization mass spectrometry to explore the in vitro metabolism of cyanoalkyl piperidine derivatives by Kantharaj, E., Ehmer, Peter B., De Wagter, Katie, Tuytelaars, An, Proost, Pascale E. A., Mackie, Claire, Gilissen, Ron A. H. J.

“…A LC/MS method using atmospheric pressure chemical ionization, positive ion mode and full scan to measure the in vitro metabolic stability of cyanoalkyl…”
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Phenol sulphotransferase SULT1A1 polymorphism: molecular diagnosis and allele frequencies in Caucasian and African populations by COUGHTRIE, Michael W. H., GILISSEN, Ron A. H. J., SHEK, Benedicte, STRANGE, Richard C., FRYER, Anthony A., JONES, Peter W., BAMBER, Dianne E.

“…Sulphation, catalysed by members of the sulphotransferase (SULT) enzyme family, is an important component of the body's chemical defence mechanism, but also…”
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Phenol sulphotransferase SULT1A11 genotype is associated with reduced risk of colorectal cancer by BAMBER, Dianne E, FRYER, Anthony A, STRANGE, Richard C, ELDER, James B, DEAKIN, Mark, RAJAGOPAL, Ramesh, FAWOLE, Adeshina, GILISSEN, Ron A. H. J, CAMPBELL, F. Charles, COUGHTRIE, Michael W. H

“…Sulphation is an important detoxification pathway for numerous xenobiotics; however, it also plays an important role in the metabolism and bioactivation of…”
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The use of liquid chromatography-atmospheric pressure chemical ionization mass spectrometry to explore thein vitro metabolism of cyanoalkyl piperidine derivatives by Kantharaj, E., Ehmer, Peter B., De Wagter, Katie, Tuytelaars, An, Proost, Pascale E. A., Mackie, Claire, Gilissen, Ron A. H. J.

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