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Page 1
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T. Oubrie A, et al. Among authors: de zwart e, de roos j, de kimpe v. Bioorg Med Chem Lett. 2012 Jan 1;22(1):613-8. doi: 10.1016/j.bmcl.2011.10.071. Epub 2011 Nov 3. Bioorg Med Chem Lett. 2012. PMID: 22119462
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Kaptein A, Oubrie A, de Zwart E, Hoogenboom N, de Wit J, van de Kar B, van Hoek M, Vogel G, de Kimpe V, Schultz-Fademrecht C, Borsboom J, van Zeeland M, Versteegh J, Kazemier B, de Roos J, Wijnands F, Dulos J, Jaeger M, Leandro-Garcia P, Barf T. Kaptein A, et al. Among authors: de zwart e, de roos j, de wit j, de kimpe v. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3823-7. doi: 10.1016/j.bmcl.2011.04.016. Epub 2011 Apr 16. Bioorg Med Chem Lett. 2011. PMID: 21565498
Structure-based lead identification of ATP-competitive MK2 inhibitors.
Barf T, Kaptein A, de Wilde S, van der Heijden R, van Someren R, Demont D, Schultz-Fademrecht C, Versteegh J, van Zeeland M, Seegers N, Kazemier B, van de Kar B, van Hoek M, de Roos J, Klop H, Smeets R, Hofstra C, Hornberg J, Oubrie A. Barf T, et al. Among authors: de wilde s, de roos j. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3818-22. doi: 10.1016/j.bmcl.2011.04.018. Epub 2011 Apr 16. Bioorg Med Chem Lett. 2011. PMID: 21565500
Discovery and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists.
van der Stelt M, Cals J, Broeders-Josten S, Cottney J, van der Doelen AA, Hermkens M, de Kimpe V, King A, Klomp J, Oosterom J, Pols-de Rooij I, de Roos J, van Tilborg M, Boyce S, Baker J. van der Stelt M, et al. Among authors: de roos j, de kimpe v. J Med Chem. 2011 Oct 27;54(20):7350-62. doi: 10.1021/jm200916p. Epub 2011 Sep 29. J Med Chem. 2011. PMID: 21923175
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. Uitdehaag JCM, et al. Among authors: de man j, de wit jjp, de vetter jrf, de roos jadm. J Mol Biol. 2017 Jul 7;429(14):2211-2230. doi: 10.1016/j.jmb.2017.05.014. Epub 2017 May 21. J Mol Biol. 2017. PMID: 28539250
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. Zaman GJR, et al. Among authors: de man j, de roos jadm. Mol Cancer Ther. 2017 Nov;16(11):2609-2617. doi: 10.1158/1535-7163.MCT-17-0342. Epub 2017 Jul 27. Mol Cancer Ther. 2017. PMID: 28751540
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. Libouban MAA, et al. Among authors: de man j, de roos jadm. Oncotarget. 2017 Jun 13;8(24):38309-38325. doi: 10.18632/oncotarget.16213. Oncotarget. 2017. PMID: 28415765 Free PMC article.
Comparative kinase and cancer cell panel profiling of kinase inhibitors approved for clinical use from 2018 to 2020.
Kooijman JJ, van Riel WE, Dylus J, Prinsen MBW, Grobben Y, de Bitter TJJ, van Doornmalen AM, Melis JJTM, Uitdehaag JCM, Narumi Y, Kawase Y, de Roos JADM, Willemsen-Seegers N, Zaman GJR. Kooijman JJ, et al. Among authors: de roos jadm. Front Oncol. 2022 Sep 14;12:953013. doi: 10.3389/fonc.2022.953013. eCollection 2022. Front Oncol. 2022. PMID: 36185300 Free PMC article.
Cryopreserved cells facilitate cell-based drug discovery.
Zaman GJ, de Roos JA, Blomenröhr M, van Koppen CJ, Oosterom J. Zaman GJ, et al. Among authors: de roos ja. Drug Discov Today. 2007 Jul;12(13-14):521-6. doi: 10.1016/j.drudis.2007.05.008. Epub 2007 Jun 27. Drug Discov Today. 2007. PMID: 17631245 Review.
42 results