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Items: 8

1.

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.

PMID:
30381447
2.

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

Walter NM, Wentsch HK, Bührmann M, Bauer SM, Döring E, Mayer-Wrangowski S, Sievers-Engler A, Willemsen-Seegers N, Zaman G, Buijsman R, Lämmerhofer M, Rauh D, Laufer SA.

J Med Chem. 2017 Oct 12;60(19):8027-8054. doi: 10.1021/acs.jmedchem.7b00745. Epub 2017 Sep 7.

PMID:
28834431
3.

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.

PMID:
28539250
4.

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.

5.

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.

PMID:
28397331
6.

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.

PMID:
28043854
7.

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.

8.

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.

PMID:
26153498

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