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Structural investigation of B-Raf paradox breaker and inducer inhibitors.
Arora R, Di Michele M, Stes E, Vandermarliere E, Martens L, Gevaert K, Van Heerde E, Linders JT, Brehmer D, Jacoby E, Bonnet P. Arora R, et al. J Med Chem. 2015 Feb 26;58(4):1818-31. doi: 10.1021/jm501667n. Epub 2015 Feb 10. J Med Chem. 2015. PMID: 25611072
Limited Proteolysis Combined with Stable Isotope Labeling Reveals Conformational Changes in Protein (Pseudo)kinases upon Binding Small Molecules.
Di Michele M, Stes E, Vandermarliere E, Arora R, Astorga-Wells J, Vandenbussche J, van Heerde E, Zubarev R, Bonnet P, Linders JT, Jacoby E, Brehmer D, Martens L, Gevaert K. Di Michele M, et al. J Proteome Res. 2015 Oct 2;14(10):4179-93. doi: 10.1021/acs.jproteome.5b00282. Epub 2015 Aug 25. J Proteome Res. 2015. PMID: 26293246
Correction: MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.
Beke L, Kig C, Linders JTM, Boens S, Boeckx A, van Heerde E, Parade M, De Bondt A, Van den Wyngaert I, Bashir T, Ogata S, Meerpoel L, Van Eynde A, Johnson CN, Beullens M, Brehmer D, Bollen M. Beke L, et al. Biosci Rep. 2018 Nov 30;38(6):BSR-20150194_COR. doi: 10.1042/BSR-20150194_COR. Print 2018 Dec 21. Biosci Rep. 2018. PMID: 30504271 Free PMC article. No abstract available.
Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity.
Brehmer D, Beke L, Wu T, Millar HJ, Moy C, Sun W, Mannens G, Pande V, Boeckx A, van Heerde E, Nys T, Gustin EM, Verbist B, Zhou L, Fan Y, Bhargava V, Safabakhsh P, Vinken P, Verhulst T, Gilbert A, Rai S, Graubert TA, Pastore F, Fiore D, Gu J, Johnson A, Philippar U, Morschhäuser B, Walker D, De Lange D, Keersmaekers V, Viellevoye M, Diels G, Schepens W, Thuring JW, Meerpoel L, Packman K, Lorenzi MV, Laquerre S. Brehmer D, et al. Mol Cancer Ther. 2021 Dec;20(12):2317-2328. doi: 10.1158/1535-7163.MCT-21-0367. Epub 2021 Sep 28. Mol Cancer Ther. 2021. PMID: 34583982 Free PMC article.
11 results