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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: kazemier b. 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: kazemier b. 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: kazemier b. 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
X-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11β-substituted steroids.
Lusher SJ, Raaijmakers HC, Vu-Pham D, Kazemier B, Bosch R, McGuire R, Azevedo R, Hamersma H, Dechering K, Oubrie A, van Duin M, de Vlieg J. Lusher SJ, et al. Among authors: kazemier b. J Biol Chem. 2012 Jun 8;287(24):20333-43. doi: 10.1074/jbc.M111.308403. Epub 2012 Apr 25. J Biol Chem. 2012. PMID: 22535964 Free PMC article.
A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. Jamieson C, et al. Among authors: kazemier b. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6072-5. doi: 10.1016/j.bmcl.2010.08.063. Epub 2010 Aug 15. Bioorg Med Chem Lett. 2010. PMID: 20817521 Free article.
A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies.
Jamieson C, Basten S, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Moir EM, Morrow JA, Papakosta M, Rankovic Z, Smith L. Jamieson C, et al. Among authors: kazemier b. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5753-6. doi: 10.1016/j.bmcl.2010.07.138. Epub 2010 Aug 13. Bioorg Med Chem Lett. 2010. PMID: 20805031 Free article.
High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.
Fradera X, Kazemier B, Carswell E, Cooke A, Oubrie A, Hamilton W, Dempster M, Krapp S, Nagel S, Jestel A. Fradera X, et al. Among authors: kazemier b. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Apr 1;68(Pt 4):404-8. doi: 10.1107/S1744309112009037. Epub 2012 Mar 27. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012. PMID: 22505407 Free PMC article.
Structure based evolution of a novel series of positive modulators of the AMPA receptor.
Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L. Jamieson C, et al. Among authors: kazemier b. Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. doi: 10.1016/j.bmcl.2010.11.098. Epub 2010 Nov 25. Bioorg Med Chem Lett. 2011. PMID: 21190850 Free article.
74 results