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301 results

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Page 1
Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis.
van der Wel T, Hilhorst R, den Dulk H, van den Hooven T, Prins NM, Wijnakker JAPM, Florea BI, Lenselink EB, van Westen GJP, Ruijtenbeek R, Overkleeft HS, Kaptein A, Barf T, van der Stelt M. van der Wel T, et al. Among authors: kaptein a. Nat Commun. 2020 Jun 25;11(1):3216. doi: 10.1038/s41467-020-17027-5. Nat Commun. 2020. PMID: 32587248 Free PMC article.
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.
Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, van Hoek M, de Zwart E, Mittag D, Demont D, Verkaik S, Krantz F, Pearson PG, Ulrich R, Kaptein A. Barf T, et al. Among authors: kaptein a. J Pharmacol Exp Ther. 2017 Nov;363(2):240-252. doi: 10.1124/jpet.117.242909. Epub 2017 Sep 7. J Pharmacol Exp Ther. 2017. PMID: 28882879
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
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
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 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
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
Preclinical Evaluation of the Novel BTK Inhibitor Acalabrutinib in Canine Models of B-Cell Non-Hodgkin Lymphoma.
Harrington BK, Gardner HL, Izumi R, Hamdy A, Rothbaum W, Coombes KR, Covey T, Kaptein A, Gulrajani M, Van Lith B, Krejsa C, Coss CC, Russell DS, Zhang X, Urie BK, London CA, Byrd JC, Johnson AJ, Kisseberth WC. Harrington BK, et al. Among authors: kaptein a. PLoS One. 2016 Jul 19;11(7):e0159607. doi: 10.1371/journal.pone.0159607. eCollection 2016. PLoS One. 2016. PMID: 27434128 Free PMC article. Clinical Trial.
301 results