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Page 1
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: lastant j. 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
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: lastant j. 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. Among authors: lastant j. 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
Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease.
Langrish CL, Bradshaw JM, Francesco MR, Owens TD, Xing Y, Shu J, LaStant J, Bisconte A, Outerbridge C, White SD, Hill RJ, Brameld KA, Goldstein DM, Nunn PA. Langrish CL, et al. Among authors: lastant j. J Immunol. 2021 Apr 1;206(7):1454-1468. doi: 10.4049/jimmunol.2001130. Epub 2021 Mar 5. J Immunol. 2021. PMID: 33674445 Free PMC article.
Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase.
Mina-Osorio P, LaStant J, Keirstead N, Whittard T, Ayala J, Stefanova S, Garrido R, Dimaano N, Hilton H, Giron M, Lau KY, Hang J, Postelnek J, Kim Y, Min S, Patel A, Woods J, Ramanujam M, DeMartino J, Narula S, Xu D. Mina-Osorio P, et al. Among authors: lastant j. Arthritis Rheum. 2013 Sep;65(9):2380-91. doi: 10.1002/art.38047. Arthritis Rheum. 2013. PMID: 23754328 Free article.
Selective Btk inhibition by PRN1008/PRN473 blocks human CLEC-2, and PRN473 reduces venous thrombosis formation in mice.
Smith CW, Campos J, Brown HC, Jooss NJ, Ivanova VS, Harbi M, Garcia-Quintanilla L, Jossi S, Perez-Toledo M, Rookes K, Brill A, Theodore LN, Owens T, LaStant J, Foulke MC, Mukai S, Francesco M, Storek M, Hicks A, Langrish C, Nunn PA, Cunningham AF, Chauhan A, Thomas MR, Watson SP, Nicolson PLR. Smith CW, et al. Among authors: lastant j. Blood Adv. 2024 Nov 12;8(21):5557-5570. doi: 10.1182/bloodadvances.2024012713. Blood Adv. 2024. PMID: 38968150 Free PMC article.