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Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.
Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV. Perera TPS, et al. Among authors: gilissen r. Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24. Mol Cancer Ther. 2017. PMID: 28341788
JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity.
Arts J, King P, Mariën A, Floren W, Beliën A, Janssen L, Pilatte I, Roux B, Decrane L, Gilissen R, Hickson I, Vreys V, Cox E, Bol K, Talloen W, Goris I, Andries L, Du Jardin M, Janicot M, Page M, van Emelen K, Angibaud P. Arts J, et al. Among authors: gilissen r. Clin Cancer Res. 2009 Nov 15;15(22):6841-51. doi: 10.1158/1078-0432.CCR-09-0547. Epub 2009 Oct 27. Clin Cancer Res. 2009. PMID: 19861438
Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors.
Angibaud P, Van Emelen K, Decrane L, van Brandt S, Ten Holte P, Pilatte I, Roux B, Poncelet V, Speybrouck D, Queguiner L, Gaurrand S, Mariën A, Floren W, Janssen L, Verdonck M, van Dun J, van Gompel J, Gilissen R, Mackie C, Du Jardin M, Peeters J, Noppe M, Van Hijfte L, Freyne E, Page M, Janicot M, Arts J. Angibaud P, et al. Among authors: gilissen r. Bioorg Med Chem Lett. 2010 Jan 1;20(1):294-8. doi: 10.1016/j.bmcl.2009.10.118. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2010. PMID: 19906529
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: gilissen ra. 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.
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: gilissen ra. 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.
Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2.
Buntinx M, Hermans B, Goossens J, Moechars D, Gilissen RA, Doyon J, Boeckx S, Coesemans E, Van Lommen G, Van Wauwe JP. Buntinx M, et al. J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. doi: 10.1124/jpet.108.140723. Epub 2008 Jul 3. J Pharmacol Exp Ther. 2008. PMID: 18599682
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L. Lu T, et al. Among authors: gilissen r. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2159-2164. doi: 10.1016/j.bmcl.2018.05.014. Epub 2018 May 8. Bioorg Med Chem Lett. 2018. PMID: 29779975
86 results