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Page 1
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.
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, McMenamin R, Patel S, Rees DC, Sharff A, Sommen F, Wu T, Linders JT. Johnson CN, et al. Among authors: brehmer d. ACS Med Chem Lett. 2014 May 23;6(1):25-30. doi: 10.1021/ml5001245. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589925 Free PMC article.
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Johnson CN, Adelinet C, Berdini V, Beke L, Bonnet P, Brehmer D, Calo F, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA, Hamlett CC, Howard S, Meerpoel L, Mevellec L, McMenamin R, Pasquier E, Patel S, Rees DC, Linders JT. Johnson CN, et al. Among authors: brehmer d. ACS Med Chem Lett. 2014 May 23;6(1):31-6. doi: 10.1021/ml5001273. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589926 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: brehmer d. Biosci Rep. 2015 Oct 2;35(6):e00267. doi: 10.1042/BSR20150194. Biosci Rep. 2015. PMID: 26431963 Free PMC article.
Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.
Janes MR, Zhang J, Li LS, Hansen R, Peters U, Guo X, Chen Y, Babbar A, Firdaus SJ, Darjania L, Feng J, Chen JH, Li S, Li S, Long YO, Thach C, Liu Y, Zarieh A, Ely T, Kucharski JM, Kessler LV, Wu T, Yu K, Wang Y, Yao Y, Deng X, Zarrinkar PP, Brehmer D, Dhanak D, Lorenzi MV, Hu-Lowe D, Patricelli MP, Ren P, Liu Y. Janes MR, et al. Among authors: brehmer d. Cell. 2018 Jan 25;172(3):578-589.e17. doi: 10.1016/j.cell.2018.01.006. Cell. 2018. PMID: 29373830 Free 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: brehmer d. 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.
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.
Pande V, Sun W, Beke L, Berthelot D, Brehmer D, Brown D, Corbera J, Irving S, Meerpoel L, Nys T, Parade M, Robinson C, Sommen C, Viellevoye M, Wu T, Thuring JW. Pande V, et al. Among authors: brehmer d. ACS Med Chem Lett. 2020 Sep 28;11(11):2227-2231. doi: 10.1021/acsmedchemlett.0c00355. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214833 Free PMC article.
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: brehmer d. J Med Chem. 2015 Feb 26;58(4):1818-31. doi: 10.1021/jm501667n. Epub 2015 Feb 10. J Med Chem. 2015. PMID: 25611072
55 results