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Items: 27

1.

Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.

de Witte WE, Wong YC, Nederpelt I, Heitman LH, Danhof M, van der Graaf PH, Gilissen RA, de Lange EC.

Expert Opin Drug Discov. 2016;11(1):45-63. doi: 10.1517/17460441.2016.1100163. Epub 2015 Oct 20. Review.

PMID:
26484747
2.

Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.

Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8.

3.

Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.

Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT.

ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8.

4.

Towards a better prediction of peak concentration, volume of distribution and half-life after oral drug administration in man, using allometry.

Sinha VK, Vaarties K, De Buck SS, Fenu LA, Nijsen M, Gilissen RA, Sanderson W, Van Uytsel K, Hoeben E, Van Peer A, Mackie CE, Smit JW.

Clin Pharmacokinet. 2011 May;50(5):307-18. doi: 10.2165/11539250-000000000-00000.

PMID:
21456631
5.

Cardio-vascular safety beyond hERG: in silico modelling of a guinea pig right atrium assay.

Fenu LA, Teisman A, De Buck SS, Sinha VK, Gilissen RA, Nijsen MJ, Mackie CE, Sanderson WE.

J Comput Aided Mol Des. 2009 Dec;23(12):883-95. doi: 10.1007/s10822-009-9306-z. Epub 2009 Nov 5.

PMID:
19890608
6.

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.

Buntinx M, Hermans B, Goossens J, Moechars D, Gilissen RA, Doyon J, Boeckx S, Coesemans E, Van Lommen G, Van Wauwe JP.

J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. doi: 10.1124/jpet.108.140723. Epub 2008 Jul 3.

PMID:
18599682
7.

Discovery of potent, orally bioavailable small-molecule inhibitors of the human CCR2 receptor.

Doyon J, Coesemans E, Boeckx S, Buntinx M, Hermans B, Van Wauwe JP, Gilissen RA, De Groot AH, Corens D, Van Lommen G.

ChemMedChem. 2008 Apr;3(4):660-9. doi: 10.1002/cmdc.200700276.

PMID:
18188859
8.

Predicting oral clearance in humans: how close can we get with allometry?

Sinha VK, De Buck SS, Fenu LA, Smit JW, Nijsen M, Gilissen RA, Van Peer A, Lavrijsen K, Mackie CE.

Clin Pharmacokinet. 2008;47(1):35-45.

PMID:
18076217
9.

Prediction of human pharmacokinetics using physiologically based modeling: a retrospective analysis of 26 clinically tested drugs.

De Buck SS, Sinha VK, Fenu LA, Nijsen MJ, Mackie CE, Gilissen RA.

Drug Metab Dispos. 2007 Oct;35(10):1766-80. Epub 2007 Jul 9.

PMID:
17620347
10.

A single hERG mutation underlying a spectrum of acquired and congenital long QT syndrome phenotypes.

Saenen JB, Paulussen AD, Jongbloed RJ, Marcelis CL, Gilissen RA, Aerssens J, Snyders DJ, Raes AL.

J Mol Cell Cardiol. 2007 Jul;43(1):63-72. Epub 2007 May 4.

PMID:
17531263
11.
12.

Chiral capillary electrophoretic analysis of verapamil metabolism by cytochrome P450 3A4.

Ha PT, Sluyts I, Van Dyck S, Zhang J, Gilissen RA, Hoogmartens J, VanSchepdael A.

J Chromatogr A. 2006 Jul 7;1120(1-2):94-101. Epub 2005 Dec 27.

PMID:
16376901
13.

HERG mutation predicts short QT based on channel kinetics but causes long QT by heterotetrameric trafficking deficiency.

Paulussen AD, Raes A, Jongbloed RJ, Gilissen RA, Wilde AA, Snyders DJ, Smeets HJ, Aerssens J.

Cardiovasc Res. 2005 Aug 15;67(3):467-75.

PMID:
15958262
14.
15.

The use of liquid chromatography-atmospheric pressure chemical ionization mass spectrometry to explore the in vitro metabolism of cyanoalkyl piperidine derivatives.

Kantharaj E, Ehmer PB, De Wagter K, Tuytelaars A, Proost PE, Mackie C, Gilissen RA.

Biomed Chromatogr. 2005 Apr;19(3):245-9.

PMID:
15627277
16.

Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients.

Paulussen AD, Gilissen RA, Armstrong M, Doevendans PA, Verhasselt P, Smeets HJ, Schulze-Bahr E, Haverkamp W, Breithardt G, Cohen N, Aerssens J.

J Mol Med (Berl). 2004 Mar;82(3):182-8. Epub 2004 Feb 4.

PMID:
14760488
17.

Simultaneous measurement of drug metabolic stability and identification of metabolites using ion-trap mass spectrometry.

Kantharaj E, Tuytelaars A, Proost PE, Ongel Z, Van Assouw HP, Gilissen RA.

Rapid Commun Mass Spectrom. 2003;17(23):2661-8.

PMID:
14648905
18.

Phenol sulphotransferase SULT1A1*1 genotype is associated with reduced risk of colorectal cancer.

Bamber DE, Fryer AA, Strange RC, Elder JB, Deakin M, Rajagopal R, Fawole A, Gilissen RA, Campbell FC, Coughtrie MW.

Pharmacogenetics. 2001 Nov;11(8):679-85.

PMID:
11692076
19.

Identification of UDP-glucuronosyltransferases involved in the human hepatic metabolism of GV150526, a novel glycine antagonist.

Gilissen RA, Barnaby RJ, Kajbaf M.

Drug Metabol Drug Interact. 2000;16(3):173-89.

PMID:
11116752
20.

Human hepatic metabolism of a novel 2-carboxyindole glycine antagonist for stroke: in vitro-in vivo correlations.

Gilissen RA, Ferrari L, Barnaby RJ, Kajbaf M.

Xenobiotica. 2000 Sep;30(9):843-56.

PMID:
11055263
21.

Phenol sulphotransferase SULT1A1 polymorphism: molecular diagnosis and allele frequencies in Caucasian and African populations.

Coughtrie MW, Gilissen RA, Shek B, Strange RC, Fryer AA, Jones PW, Bamber DE.

Biochem J. 1999 Jan 1;337 ( Pt 1):45-9.

22.

Sulphation of N-hydroxy-4-aminobiphenyl and N-hydroxy-4-acetylaminobiphenyl by human foetal and neonatal sulphotransferase.

Gilissen RA, Hume R, Meerman JH, Coughtrie MW.

Biochem Pharmacol. 1994 Aug 17;48(4):837-40.

PMID:
8080456
23.
24.

Sulfation of aromatic hydroxamic acids and hydroxylamines by multiple forms of human liver sulfotransferases.

Gilissen RA, Bamforth KJ, Stavenuiter JF, Coughtrie MW, Meerman JH.

Carcinogenesis. 1994 Jan;15(1):39-45.

PMID:
8293546
25.

Sulfation of hydroxylamines and hydroxamic acids in liver cytosol from male and female rats and purified aryl sulfotransferase IV.

Gilissen RA, Ringer DP, Stavenuiter HJ, Mulder GJ, Meerman JH.

Carcinogenesis. 1992 Oct;13(10):1699-703.

PMID:
1423828
26.

Immobilization of solubilized UDP-glucuronosyltransferase from rat liver microsomes to Sepharose 4B.

Gilissen RA, Meerman JH, Mulder GJ.

Biochem Pharmacol. 1992 Jun 23;43(12):2661-3.

PMID:
1632822

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