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Combined cellular and biochemical profiling to identify predictive drug response biomarkers for kinase inhibitors approved for clinical use between 2013 and 2017.

Uitdehaag JCM, Kooijman JJ, de Roos JADM, Prinsen MBW, Dylus J, Willemsen-Seegers N, Kawase Y, Sawa M, de Man J, van Gerwen SJC, Buijsman RC, Zaman GJR.

Mol Cancer Ther. 2018 Oct 31. pii: molcanther.0877.2018. doi: 10.1158/1535-7163.MCT-18-0877. [Epub ahead of print]


Quantitative proteomic and phosphoproteomic comparison of human colon cancer DLD-1 cells differing in ploidy and chromosome stability.

Viganó C, von Schubert C, Ahrné E, Schmidt A, Lorber T, Bubendorf L, De Vetter JRF, Zaman GJR, Storchova Z, Nigg EA.

Mol Biol Cell. 2018 May 1;29(9):1031-1047. doi: 10.1091/mbc.E17-10-0577.


TTK Inhibitors as a Targeted Therapy for CTNNB1 (β-catenin) Mutant Cancers.

Zaman GJR, de Roos JADM, Libouban MAA, Prinsen MBW, de Man J, Buijsman RC, Uitdehaag JCM.

Mol Cancer Ther. 2017 Nov;16(11):2609-2617. doi: 10.1158/1535-7163.MCT-17-0342. Epub 2017 Jul 27.


Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity.

Uitdehaag JCM, de Man J, Willemsen-Seegers N, Prinsen MBW, Libouban MAA, Sterrenburg JG, de Wit JJP, de Vetter JRF, de Roos JADM, Buijsman RC, Zaman GJR.

J Mol Biol. 2017 Jul 7;429(14):2211-2230. doi: 10.1016/j.jmb.2017.05.014. Epub 2017 May 21.


Stable aneuploid tumors cells are more sensitive to TTK inhibition than chromosomally unstable cell lines.

Libouban MAA, de Roos JADM, Uitdehaag JCM, Willemsen-Seegers N, Mainardi S, Dylus J, de Man J, Tops B, Meijerink JPP, Storchová Z, Buijsman RC, Medema RH, Zaman GJR.

Oncotarget. 2017 Jun 13;8(24):38309-38325. doi: 10.18632/oncotarget.16213.


Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine.

Wentsch HK, Walter NM, Bührmann M, Mayer-Wrangowski S, Rauh D, Zaman GJR, Willemsen-Seegers N, Buijsman RC, Henning M, Dauch D, Zender L, Laufer S.

Angew Chem Int Ed Engl. 2017 May 2;56(19):5363-5367. doi: 10.1002/anie.201701185. Epub 2017 Apr 11.


Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.

Willemsen-Seegers N, Uitdehaag JCM, Prinsen MBW, de Vetter JRF, de Man J, Sawa M, Kawase Y, Buijsman RC, Zaman GJR.

J Mol Biol. 2017 Feb 17;429(4):574-586. doi: 10.1016/j.jmb.2016.12.019. Epub 2016 Dec 30.


IL-7 Receptor Mutations and Steroid Resistance in Pediatric T cell Acute Lymphoblastic Leukemia: A Genome Sequencing Study.

Li Y, Buijs-Gladdines JG, Canté-Barrett K, Stubbs AP, Vroegindeweij EM, Smits WK, van Marion R, Dinjens WN, Horstmann M, Kuiper RP, Buijsman RC, Zaman GJ, van der Spek PJ, Pieters R, Meijerink JP.

PLoS Med. 2016 Dec 20;13(12):e1002200. doi: 10.1371/journal.pmed.1002200. eCollection 2016 Dec.


Cell Panel Profiling Reveals Conserved Therapeutic Clusters and Differentiates the Mechanism of Action of Different PI3K/mTOR, Aurora Kinase and EZH2 Inhibitors.

Uitdehaag JC, de Roos JA, Prinsen MB, Willemsen-Seegers N, de Vetter JR, Dylus J, van Doornmalen AM, Kooijman J, Sawa M, van Gerwen SJ, de Man J, Buijsman RC, Zaman GJ.

Mol Cancer Ther. 2016 Dec;15(12):3097-3109. Epub 2016 Sep 1.


MEK and PI3K-AKT inhibitors synergistically block activated IL7 receptor signaling in T-cell acute lymphoblastic leukemia.

Canté-Barrett K, Spijkers-Hagelstein JA, Buijs-Gladdines JG, Uitdehaag JC, Smits WK, van der Zwet J, Buijsman RC, Zaman GJ, Pieters R, Meijerink JP.

Leukemia. 2016 Sep;30(9):1832-43. doi: 10.1038/leu.2016.83. Epub 2016 Apr 22.


Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model.

Maia AR, de Man J, Boon U, Janssen A, Song JY, Omerzu M, Sterrenburg JG, Prinsen MB, Willemsen-Seegers N, de Roos JA, van Doornmalen AM, Uitdehaag JC, Kops GJ, Jonkers J, Buijsman RC, Zaman GJ, Medema RH.

Ann Oncol. 2015 Oct;26(10):2180-92. doi: 10.1093/annonc/mdv293. Epub 2015 Jul 7.


Chromosomal instability, tolerance of mitotic errors and multidrug resistance are promoted by tetraploidization in human cells.

Kuznetsova AY, Seget K, Moeller GK, de Pagter MS, de Roos JA, Dürrbaum M, Kuffer C, Müller S, Zaman GJ, Kloosterman WP, Storchová Z.

Cell Cycle. 2015;14(17):2810-20. doi: 10.1080/15384101.2015.1068482.


Selective Targeting of CTNBB1-, KRAS- or MYC-Driven Cell Growth by Combinations of Existing Drugs.

Uitdehaag JC, de Roos JA, van Doornmalen AM, Prinsen MB, Spijkers-Hagelstein JA, de Vetter JR, de Man J, Buijsman RC, Zaman GJ.

PLoS One. 2015 May 27;10(5):e0125021. doi: 10.1371/journal.pone.0125021. eCollection 2015. Erratum in: PLoS One. 2015;10(6):e0132230.


Controversies in ASSAY and drug development technologies: a focus on assessing irreproducibility.

Glickman JF, Lundbäck T, Napper AD, Niles WD, Simeonov A, Weaver CD, Yin HH, Zaman GJ, Osada H.

Assay Drug Dev Technol. 2014 Oct;12(8):443-51. doi: 10.1089/adt.2014.1501.


High-throughput fluorescence-based screening assays for tryptophan-catabolizing enzymes.

Seegers N, van Doornmalen AM, Uitdehaag JC, de Man J, Buijsman RC, Zaman GJ.

J Biomol Screen. 2014 Oct;19(9):1266-74. doi: 10.1177/1087057114536616. Epub 2014 May 27.


Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use.

Uitdehaag JC, de Roos JA, van Doornmalen AM, Prinsen MB, de Man J, Tanizawa Y, Kawase Y, Yoshino K, Buijsman RC, Zaman GJ.

PLoS One. 2014 Mar 20;9(3):e92146. doi: 10.1371/journal.pone.0092146. eCollection 2014.


Chemokine cooperativity is caused by competitive glycosaminoglycan binding.

Verkaar F, van Offenbeek J, van der Lee MMC, van Lith LHCJ, Watts AO, Rops ALWMM, Aguilar DC, Ziarek JJ, van der Vlag J, Handel TM, Volkman BF, Proudfoot AEI, Vischer HF, Zaman GJR, Smit MJ.

J Immunol. 2014 Apr 15;192(8):3908-3914. doi: 10.4049/jimmunol.1302159. Epub 2014 Mar 17.


β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.

Watts AO, Verkaar F, van der Lee MM, Timmerman CA, Kuijer M, van Offenbeek J, van Lith LH, Smit MJ, Leurs R, Zaman GJ, Vischer HF.

J Biol Chem. 2013 Mar 8;288(10):7169-81. doi: 10.1074/jbc.M112.406108. Epub 2013 Jan 22.


Identification and profiling of CXCR3-CXCR4 chemokine receptor heteromer complexes.

Watts AO, van Lipzig MM, Jaeger WC, Seeber RM, van Zwam M, Vinet J, van der Lee MM, Siderius M, Zaman GJ, Boddeke HW, Smit MJ, Pfleger KD, Leurs R, Vischer HF.

Br J Pharmacol. 2013 Apr;168(7):1662-74. doi: 10.1111/bph.12064.


β-Arrestin-biased signaling of PTH analogs of the type 1 parathyroid hormone receptor.

van der Lee MM, Verkaar F, Wat JW, van Offenbeek J, Timmerman M, Voorneveld L, van Lith LH, Zaman GJ.

Cell Signal. 2013 Feb;25(2):527-38. doi: 10.1016/j.cellsig.2012.11.012. Epub 2012 Nov 15.


A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.

Sanders MP, Roumen L, van der Horst E, Lane JR, Vischer HF, van Offenbeek J, de Vries H, Verhoeven S, Chow KY, Verkaar F, Beukers MW, McGuire R, Leurs R, Ijzerman AP, de Vlieg J, de Esch IJ, Zaman GJ, Klomp JP, Bender A, de Graaf C.

J Med Chem. 2012 Jun 14;55(11):5311-25. doi: 10.1021/jm300280e. Epub 2012 May 23.


A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets.

Uitdehaag JC, Verkaar F, Alwan H, de Man J, Buijsman RC, Zaman GJ.

Br J Pharmacol. 2012 Jun;166(3):858-76. doi: 10.1111/j.1476-5381.2012.01859.x. Review.


Identification of a novel allosteric binding site in the CXCR2 chemokine receptor.

de Kruijf P, Lim HD, Roumen L, Renjaän VA, Zhao J, Webb ML, Auld DS, Wijkmans JC, Zaman GJ, Smit MJ, de Graaf C, Leurs R.

Mol Pharmacol. 2011 Dec;80(6):1108-18. doi: 10.1124/mol.111.073825. Epub 2011 Sep 23.


Discovery of novel small molecule activators of β-catenin signaling.

Verkaar F, van der Stelt M, Blankesteijn WM, van der Doelen AA, Zaman GJ.

PLoS One. 2011 Apr 29;6(4):e19185. doi: 10.1371/journal.pone.0019185.


Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ.

Verkaar F, van der Doelen AA, Smits JF, Blankesteijn WM, Zaman GJ.

Chem Biol. 2011 Apr 22;18(4):485-94. doi: 10.1016/j.chembiol.2011.01.015.


A theoretical entropy score as a single value to express inhibitor selectivity.

Uitdehaag JC, Zaman GJ.

BMC Bioinformatics. 2011 Apr 12;12:94. doi: 10.1186/1471-2105-12-94.


CXCR2 antagonists block the N-Ac-PGP-induced neutrophil influx in the airways of mice, but not the production of the chemokine CXCL1.

Braber S, Overbeek SA, Koelink PJ, Henricks PA, Zaman GJ, Garssen J, Kraneveld AD, Folkerts G.

Eur J Pharmacol. 2011 Oct 15;668(3):443-9. doi: 10.1016/j.ejphar.2011.03.025. Epub 2011 Mar 31.


N-acetylated Proline-Glycine-Proline induced G-protein dependent chemotaxis of neutrophils is independent of CXCL8 release.

Overbeek SA, Henricks PA, Srienc AI, Koelink PJ, de Kruijf P, Lim HD, Smit MJ, Zaman GJ, Garssen J, Nijkamp FP, Kraneveld AD, Folkerts G.

Eur J Pharmacol. 2011 Oct 15;668(3):428-34. doi: 10.1016/j.ejphar.2011.03.022. Epub 2011 Mar 31.


New avenues to target Wnt/β-catenin signaling.

Verkaar F, Zaman GJ.

Drug Discov Today. 2011 Jan;16(1-2):35-41. doi: 10.1016/j.drudis.2010.11.007. Epub 2010 Nov 24. Review.


A model for signaling specificity of Wnt/Frizzled combinations through co-receptor recruitment.

Verkaar F, Zaman GJ.

FEBS Lett. 2010 Sep 24;584(18):3850-4. doi: 10.1016/j.febslet.2010.08.030. Epub 2010 Aug 25.


The collagen-breakdown product N-acetyl-Proline-Glycine-Proline (N-alpha-PGP) does not interact directly with human CXCR1 and CXCR2.

de Kruijf P, Lim HD, Overbeek SA, Zaman GJ, Kraneveld AD, Folkerts G, Leurs R, Smit MJ.

Eur J Pharmacol. 2010 Sep 15;643(1):29-33. doi: 10.1016/j.ejphar.2010.06.017. Epub 2010 Jun 21.


beta-Galactosidase enzyme fragment complementation for the measurement of Wnt/beta-catenin signaling.

Verkaar F, Blankesteijn WM, Smits JF, Zaman GJ.

FASEB J. 2010 Apr;24(4):1205-17. doi: 10.1096/fj.09-141671. Epub 2009 Nov 25.


C5a-stimulated recruitment of beta-arrestin2 to the nonsignaling 7-transmembrane decoy receptor C5L2.

Van Lith LH, Oosterom J, Van Elsas A, Zaman GJ.

J Biomol Screen. 2009 Oct;14(9):1067-75. doi: 10.1177/1087057109341407. Epub 2009 Jul 29.


Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1.

van der Lee MM, Blomenröhr M, van der Doelen AA, Wat JW, Smits N, Hanson BJ, van Koppen CJ, Zaman GJ.

J Biomol Screen. 2009 Aug;14(7):811-23. doi: 10.1177/1087057109337937. Epub 2009 Jun 11.


Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.

de Kruijf P, van Heteren J, Lim HD, Conti PG, van der Lee MM, Bosch L, Ho KK, Auld D, Ohlmeyer M, Smit MJ, Wijkmans JC, Zaman GJ, Smit MJ, Leurs R.

J Pharmacol Exp Ther. 2009 May;329(2):783-90. doi: 10.1124/jpet.108.148387. Epub 2009 Feb 3. Erratum in: J Pharmacol Exp Ther. 2009 Jul;330(1):367.


Characterization and optimization of a red-shifted fluorescence polarization ADP detection assay.

Kleman-Leyer KM, Klink TA, Kopp AL, Westermeyer TA, Koeff MD, Larson BR, Worzella TJ, Pinchard CA, van de Kar SA, Zaman GJ, Hornberg JJ, Lowery RG.

Assay Drug Dev Technol. 2009 Feb;7(1):56-67. doi: 10.1089/adt.2008.175.


beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1.

van Der Lee MM, Bras M, van Koppen CJ, Zaman GJ.

J Biomol Screen. 2008 Dec;13(10):986-98. doi: 10.1177/1087057108326144. Epub 2008 Nov 25.


Stably overexpressed human Frizzled-2 signals through the beta-catenin pathway and does not activate Ca2+-mobilization in Human Embryonic Kidney 293 cells.

Verkaar F, van Rosmalen JW, Smits JF, Blankesteijn WM, Zaman GJ.

Cell Signal. 2009 Jan;21(1):22-33. doi: 10.1016/j.cellsig.2008.09.008. Epub 2008 Sep 25.


Cell-based screening.

Zaman GJ.

Comb Chem High Throughput Screen. 2008 Aug;11(7):494. No abstract available.


G protein-independent cell-based assays for drug discovery on seven-transmembrane receptors.

Verkaar F, van Rosmalen JW, Blomenröhr M, van Koppen CJ, Blankesteijn WM, Smits JF, Zaman GJ.

Biotechnol Annu Rev. 2008;14:253-74. doi: 10.1016/S1387-2656(08)00010-0. Review.


A signaling-selective, nanomolar potent allosteric low molecular weight agonist for the human luteinizing hormone receptor.

van Koppen CJ, Zaman GJ, Timmers CM, Kelder J, Mosselman S, van de Lagemaat R, Smit MJ, Hanssen RG.

Naunyn Schmiedebergs Arch Pharmacol. 2008 Nov;378(5):503-14. doi: 10.1007/s00210-008-0318-3. Epub 2008 Jun 13.


Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors.

Verzijl D, Storelli S, Scholten DJ, Bosch L, Reinhart TA, Streblow DN, Tensen CP, Fitzsimons CP, Zaman GJ, Pease JE, de Esch IJ, Smit MJ, Leurs R.

J Pharmacol Exp Ther. 2008 May;325(2):544-55. doi: 10.1124/jpet.107.134783. Epub 2008 Feb 12.


Ligand-induced folding of the guanine-sensing riboswitch is controlled by a combined predetermined induced fit mechanism.

Ottink OM, Rampersad SM, Tessari M, Zaman GJ, Heus HA, Wijmenga SS.

RNA. 2007 Dec;13(12):2202-12. Epub 2007 Oct 24.


Cryopreserved cells facilitate cell-based drug discovery.

Zaman GJ, de Roos JA, Blomenröhr M, van Koppen CJ, Oosterom J.

Drug Discov Today. 2007 Jul;12(13-14):521-6. Epub 2007 Jun 27. Review.


Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors.

Zaman GJ, van der Lee MM, Kok JJ, Nelissen RL, Loomans EE.

Assay Drug Dev Technol. 2006 Aug;4(4):411-20.


Screening for Modulators of G Protein-Coupled Receptors.

Zaman GJ.

Comb Chem High Throughput Screen. 2005 Jun;8(4):283. No abstract available.


Cell-based screening.

Zaman GJ.

Drug Discov Today. 2004 Oct 1;9(19):828-30. No abstract available.


High-throughput screening with immobilized metal ion affinity-based fluorescence polarization detection, a homogeneous assay for protein kinases.

Loomans EE, van Doornmalen AM, Wat JW, Zaman GJ.

Assay Drug Dev Technol. 2003 Jun;1(3):445-53.


Fluorescence assays for high-throughput screening of protein kinases.

Zaman GJ, Garritsen A, de Boer T, van Boeckel CA.

Comb Chem High Throughput Screen. 2003 Jun;6(4):313-20. Review.


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