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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. Among authors: van heerde e. 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.
MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.
Beke L, Kig C, Linders JT, 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. Among authors: van heerde e. Biosci Rep. 2015 Oct 2;35(6):e00267. doi: 10.1042/BSR20150194. Biosci Rep. 2015. PMID: 26431963 Free PMC article.
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. Among authors: van heerde e. 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.
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. Among authors: van heerde e. 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
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. Among authors: van heerde e. J Med Chem. 2015 Feb 26;58(4):1818-31. doi: 10.1021/jm501667n. Epub 2015 Feb 10. J Med Chem. 2015. PMID: 25611072
Correction to 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. Among authors: van heerde e. J Med Chem. 2016 Jul 28;59(14):6973. doi: 10.1021/acs.jmedchem.6b00941. Epub 2016 Jul 6. J Med Chem. 2016. PMID: 27385554 No abstract available.
12 results