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Tumour necrosis factor-alpha stimulates dehydroepiandrosterone metabolism in human fibroblast-like synoviocytes: a role for nuclear factor-kappaB and activator protein-1 in the regulation of expression of cytochrome p450 enzyme 7b.
Dulos J, Kaptein A, Kavelaars A, Heijnen C, Boots A. Dulos J, et al. Among authors: kaptein a. Arthritis Res Ther. 2005;7(6):R1271-80. doi: 10.1186/ar1819. Epub 2005 Sep 15. Arthritis Res Ther. 2005. PMID: 16277680 Free PMC article.
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. 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
In vivo knockdown of TAK1 accelerates bone marrow proliferation/differentiation and induces systemic inflammation.
Vink PM, Smout WM, Driessen-Engels LJ, de Bruin AM, Delsing D, Krajnc-Franken MA, Jansen AJ, Rovers EF, van Puijenbroek AA, Kaptein A, Nolte MA, Garritsen A, van Eenennaam H. Vink PM, et al. Among authors: kaptein a. PLoS One. 2013;8(3):e57348. doi: 10.1371/journal.pone.0057348. Epub 2013 Mar 7. PLoS One. 2013. PMID: 23505428 Free PMC article.
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: kaptein a. 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
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: kaptein a. 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 quinoline-based irreversible BTK inhibitors.
de Bruin G, Demont D, de Zwart E, Verkaik S, Hoogenboom N, van de Kar B, van Lith B, Emmelot-van Hoek M, Gulrajani M, Covey T, Kaptein A, Barf T. de Bruin G, et al. Among authors: kaptein a. Bioorg Med Chem Lett. 2020 Jul 15;30(14):127261. doi: 10.1016/j.bmcl.2020.127261. Epub 2020 May 13. Bioorg Med Chem Lett. 2020. PMID: 32527559
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors.
Hoogenboom N, Demont D, de Zwart E, Verkaik S, Emmelot M, van de Kar B, Kaptein A, Barf T. Hoogenboom N, et al. Among authors: kaptein a. Bioorg Med Chem Lett. 2021 Nov 15;52:128406. doi: 10.1016/j.bmcl.2021.128406. Epub 2021 Oct 5. Bioorg Med Chem Lett. 2021. PMID: 34624491
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Cai J, Baugh M, Black D, Long C, Jonathan Bennett D, Dempster M, Fradera X, Gillespie J, Andrews F, Boucharens S, Bruin J, Cameron KS, Cumming I, Hamilton W, Jones PS, Kaptein A, Kinghorn E, Maidment M, Martin I, Mitchell A, Rankovic Z, Robinson J, Scullion P, Uitdehaag JC, Vink P, Westwood P, van Zeeland M, van Berkom L, Bastiani M, Meulemans T. Cai J, et al. Among authors: kaptein a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20598883
301 results