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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: verner e. 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
Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).
Owens TD, Brameld KA, Verner EJ, Ton T, Li X, Zhu J, Masjedizadeh MR, Bradshaw JM, Hill RJ, Tam D, Bisconte A, Kim EO, Francesco M, Xing Y, Shu J, Karr D, LaStant J, Finkle D, Loewenstein N, Haberstock-Debic H, Taylor MJ, Nunn P, Langrish CL, Goldstein DM. Owens TD, et al. J Med Chem. 2022 Apr 14;65(7):5300-5316. doi: 10.1021/acs.jmedchem.1c01170. Epub 2022 Mar 18. J Med Chem. 2022. PMID: 35302767
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: verner e. 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
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: verner e. 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.
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: verner e. 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.
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.
Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA. Mackman RL, et al. Among authors: verner e. J Med Chem. 2001 Nov 8;44(23):3856-71. doi: 10.1021/jm010244+. J Med Chem. 2001. PMID: 11689072
A nonselective inhibitor of trypsin-like serine proteases, 2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine (1) (Verner, E.; Katz, B. A.; Spencer, J.; Allen, D.; Hataye, J.; Hruzewicz, W.; Hui, H. ...
A nonselective inhibitor of trypsin-like serine proteases, 2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine (1) (Verner, E …
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa.
Verner E, Katz BA, Spencer JR, Allen D, Hataye J, Hruzewicz W, Hui HC, Kolesnikov A, Li Y, Luong C, Martelli A, Radika K, Rai R, She M, Shrader W, Sprengeler PA, Trapp S, Wang J, Young WB, Mackman RL. Verner E, et al. J Med Chem. 2001 Aug 16;44(17):2753-71. doi: 10.1021/jm0100638. J Med Chem. 2001. PMID: 11495587
Development of potent and selective factor Xa inhibitors.
Rai R, Kolesnikov A, Li Y, Young WB, Leahy E, Sprengeler PA, Verner E, Shrader WD, Burgess-Henry J, Sangalang JC, Allen D, Chen X, Katz BA, Luong C, Elrod K, Cregar L. Rai R, et al. Among authors: verner e. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1797-800. doi: 10.1016/s0960-894x(01)00311-0. Bioorg Med Chem Lett. 2001. PMID: 11459634
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J. Mackman RL, et al. Among authors: verner e. Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22. doi: 10.1016/s0960-894x(02)00311-6. Bioorg Med Chem Lett. 2002. PMID: 12113832
73 results