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Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO. Brameld KA, et al. Among authors: funk jo. J Med Chem. 2017 Aug 10;60(15):6516-6527. doi: 10.1021/acs.jmedchem.7b00360. Epub 2017 Jul 25. J Med Chem. 2017. PMID: 28665128
Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J, Patel V, Ton T, Li X, Loughhead DG, Nunn PA, Karr DE, Gerritsen ME, Funk JO, Owens TD, Verner E, Brameld KA, Hill RJ, Goldstein DM, Taunton J. Bradshaw JM, et al. Among authors: funk jo. Nat Chem Biol. 2015 Jul;11(7):525-31. doi: 10.1038/nchembio.1817. Epub 2015 May 25. Nat Chem Biol. 2015. PMID: 26006010 Free PMC article.
The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance.
Venetsanakos E, Brameld KA, Phan VT, Verner E, Owens TD, Xing Y, Tam D, LaStant J, Leung K, Karr DE, Hill RJ, Gerritsen ME, Goldstein DM, Funk JO, Bradshaw JM. Venetsanakos E, et al. Among authors: funk jo. Mol Cancer Ther. 2017 Dec;16(12):2668-2676. doi: 10.1158/1535-7163.MCT-17-0309. Epub 2017 Oct 4. Mol Cancer Ther. 2017. PMID: 28978721
Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.
Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A, Owens TD, Verner E, Brameld KA, Funk JO, Hill RJ, Johnson AJ, Dubovsky JA. Zhong Y, et al. Among authors: funk jo. J Biol Chem. 2015 Mar 6;290(10):5960-78. doi: 10.1074/jbc.M114.614891. Epub 2015 Jan 15. J Biol Chem. 2015. PMID: 25593320 Free PMC article.
Psoriasis induced by interferon-alpha.
Funk J, Langeland T, Schrumpf E, Hanssen LE. Funk J, et al. Br J Dermatol. 1991 Nov;125(5):463-5. doi: 10.1111/j.1365-2133.1991.tb14774.x. Br J Dermatol. 1991. PMID: 1751354
49 results