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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. 2019 Feb;18(2):470-481. doi: 10.1158/1535-7163.MCT-18-0877. Epub 2018 Oct 31.


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.


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.


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.


Delaying aging and the aging-associated decline in protein homeostasis by inhibition of tryptophan degradation.

van der Goot AT, Zhu W, Vázquez-Manrique RP, Seinstra RI, Dettmer K, Michels H, Farina F, Krijnen J, Melki R, Buijsman RC, Ruiz Silva M, Thijssen KL, Kema IP, Neri C, Oefner PJ, Nollen EA.

Proc Natl Acad Sci U S A. 2012 Sep 11;109(37):14912-7. doi: 10.1073/pnas.1203083109. Epub 2012 Aug 27.


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.


Synthetic heparin derivatives as new anticoagulant drugs.

de Kort M, Buijsman RC, van Boeckel CA.

Drug Discov Today. 2005 Jun 1;10(11):769-79. Review.


Non-steroidal steroid receptor modulators.

Buijsman RC, Hermkens PH, van Rijn RD, Stock HT, Teerhuis NM.

Curr Med Chem. 2005;12(9):1017-75. Review.


Ruthenium-catalyzed olefin metathesis in ionic liquids.

Buijsman RC, van Vuuren E, Sterrenburg JG.

Org Lett. 2001 Nov 15;3(23):3785-7.


Synthesis of heparin-like antithrombotics having perphosphorylated thrombin binding domains.

Buijsman RC, Basten JE, Dreef-Tromp CM, van der Marel GA, van Boeckel CA, van Boom JH.

Bioorg Med Chem. 1999 Sep;7(9):1881-90.


Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.

Buijsman RC, Basten JE, van Dinther TG, van der Marel GA, van Boeckel CA, van Boom JH.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2013-8.


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