Publications by authors named "Ron Gilissen"

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Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Tianbao Lu, Carsten Schubert, Maxwell D Cummings, Gilles Bignan, Peter J Connolly, Ron Gilissen

Bioorg Med Chem Lett· July 2018

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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Timothy P S Perera, Eleonora Jovcheva, Laurence Mevellec, Jorge Vialard, Desiree De Lange, Ron Gilissen

Mol Cancer Ther· June 2017

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Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.
Wilhelmus E A de Witte, Yin Cheong Wong, Indira Nederpelt, Laura H Heitman, Meindert Danhof, Ron A H J Gilissen

Expert Opin Drug Discov· September 2016

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Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Christopher N Johnson, Valerio Berdini, Lijs Beke, Pascal Bonnet, Dirk Brehmer, Ron A H J Gilissen

ACS Med Chem Lett· January 2015

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Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Christopher N Johnson, Christophe Adelinet, Valerio Berdini, Lijs Beke, Pascal Bonnet, Ron A H J Gilissen

ACS Med Chem Lett· January 2015

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Novel antibiotics targeting respiratory ATP synthesis in Gram-positive pathogenic bacteria.
Wendy Balemans, Luc Vranckx, Nacer Lounis, Ovidiu Pop, Jérôme Guillemont, Ron Gilissen

Antimicrob Agents Chemother· August 2012

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Pharmacokinetics and pharmacodynamics of TMC207 and its N-desmethyl metabolite in a murine model of tuberculosis.
Marie-Claude Rouan, Nacer Lounis, Tom Gevers, Lieve Dillen, Ron Gilissen

Antimicrob Agents Chemother· March 2012

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Prediction of human oral plasma concentration-time profiles using preclinical data: comparative evaluation of prediction approaches in early pharmaceutical discovery.
An Van den Bergh, Vikash Sinha, Ron Gilissen, Roel Straetemans, Koen Wuyts

Clin Pharmacokinet· August 2011

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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.
Vikash K Sinha, Karin Vaarties, Stefan S De Buck, Luca A Fenu, Marjoleen Nijsen, Ron A H J Gilissen

Clin Pharmacokinet· May 2011

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Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors.
Patrick Angibaud, Kristof Van Emelen, Laurence Decrane, Sven van Brandt, Peter Ten Holte, Ron Gilissen

Bioorg Med Chem Lett· January 2010

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Essentiality of FASII pathway for Staphylococcus aureus.
Wendy Balemans, Nacer Lounis, Ron Gilissen, Jerome Guillemont, Kenny Simmen

Nature· January 2010

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Cardio-vascular safety beyond hERG: in silico modelling of a guinea pig right atrium assay.
Luca A Fenu, Ard Teisman, Stefan S De Buck, Vikash K Sinha, Ron A H J Gilissen

J Comput Aided Mol Des· December 2009

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JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity.
Janine Arts, Peter King, Ann Mariën, Wim Floren, Ann Beliën, Ron Gilissen

Clin Cancer Res· November 2009

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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.
Mieke Buntinx, Bart Hermans, Jan Goossens, Dieder Moechars, Ron A H J Gilissen

J Pharmacol Exp Ther· October 2008

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Discovery of potent, orally bioavailable small-molecule inhibitors of the human CCR2 receptor.
Julien Doyon, Erwin Coesemans, Staf Boeckx, Mieke Buntinx, Bart Hermans, Ron A H J Gilissen

ChemMedChem· April 2008

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Predicting oral clearance in humans: how close can we get with allometry?
Vikash K Sinha, Stefan S De Buck, Luca A Fenu, Johan W Smit, Marjoleen Nijsen, Ron A H J Gilissen

Clin Pharmacokinet· March 2008

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Prediction of human pharmacokinetics using physiologically based modeling: a retrospective analysis of 26 clinically tested drugs.
Stefan S De Buck, Vikash K Sinha, Luca A Fenu, Marjoleen J Nijsen, Claire E Mackie, Ron A H J Gilissen

Drug Metab Dispos· October 2007

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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.
Stefan S De Buck, Vikash K Sinha, Luca A Fenu, Ron A Gilissen, Claire E Mackie

Drug Metab Dispos· April 2007

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Chiral capillary electrophoretic analysis of verapamil metabolism by cytochrome P450 3A4.
Pham Thi Thanh Ha, Inge Sluyts, Sigrid Van Dyck, Jie Zhang, Ron A H J Gilissen

J Chromatogr A· July 2006

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HERG mutation predicts short QT based on channel kinetics but causes long QT by heterotetrameric trafficking deficiency.
Aimée D C Paulussen, Adam Raes, Roselie J Jongbloed, Ron A H J Gilissen, Arthur A M Wilde

Cardiovasc Res· August 2005

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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.
E Kantharaj, Peter B Ehmer, An Tuytelaars, Anne Van Vlaslaer, Claire Mackie, Ron A H J Gilissen

Rapid Commun Mass Spectrom· June 2005

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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.
E Kantharaj, Peter B Ehmer, Katie De Wagter, An Tuytelaars, Pascale E A Proost, Ron A H J Gilissen

Biomed Chromatogr· April 2005

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Determination of cytochrome P450 1A2 and cytochrome P450 3A4 induction in cryopreserved human hepatocytes.
Dirk Roymans, Cis Van Looveren, Angelique Leone, J Brandon Parker, Michael McMillian, Ron Gilissen

Biochem Pharmacol· February 2004

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Simultaneous measurement of drug metabolic stability and identification of metabolites using ion-trap mass spectrometry.
E Kantharaj, An Tuytelaars, Pascale E A Proost, Zuleyha Ongel, Harrie P Van Assouw, Ron A H J Gilissen

Rapid Commun Mass Spectrom· January 2004

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CYP2C8 polymorphisms in Caucasians and their relationship with paclitaxel 6alpha-hydroxylase activity in human liver microsomes.
Namrata Bahadur, Julian B S Leathart, Elaine Mutch, Dorothy Steimel-Crespi, Stuart A Dunn, Ron Gilissen

Biochem Pharmacol· December 2002

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