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Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.
Velaparthi U, Darne CP, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, Parrish K, Yang Z, Swanson J, Brown J, Dhar G, Anandam A, Holenarsipur VK, Palanisamy K, Wautlet BS, Fereshteh MP, Lippy J, Tebben AJ, Sheriff S, Ruzanov M, Yan C, Gupta A, Gupta AK, Vetrichelvan M, Mathur A, Gelman M, Singh R, Kinsella T, Murtaza A, Fargnoli J, Vite G, Borzilleri RM. Velaparthi U, et al. Among authors: augustine rauch k. ACS Med Chem Lett. 2020 Jan 28;11(2):172-178. doi: 10.1021/acsmedchemlett.9b00552. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071685 Free PMC article.
Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.
Zhang Y, Zhao Y, Tebben AJ, Sheriff S, Ruzanov M, Fereshteh MP, Fan Y, Lippy J, Swanson J, Ho CP, Wautlet BS, Rose A, Parrish K, Yang Z, Donnell AF, Zhang L, Fink BE, Vite GD, Augustine-Rauch K, Fargnoli J, Borzilleri RM. Zhang Y, et al. Among authors: augustine rauch k. ACS Med Chem Lett. 2018 Oct 17;9(11):1117-1122. doi: 10.1021/acsmedchemlett.8b00357. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429955 Free PMC article.
Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor.
Zhang Y, Parrish KE, Tortolani DR, Poss MA, Huang A, Wan H, Purandare AV, Donnell AF, Kempson J, Hou X, Pawluczyk J, Yip S, Luk E, Raghavan N, Swanson J, Smalley J, Murtaza A, Yang Z, Augustine-Rauch K, Lombardo LJ, Borzilleri R. Zhang Y, et al. Among authors: augustine rauch k. J Med Chem. 2021 Nov 11;64(21):15787-15798. doi: 10.1021/acs.jmedchem.0c02043. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704759
Zebrafish embryo developmental toxicology assay.
Panzica-Kelly JM, Zhang CX, Augustine-Rauch K. Panzica-Kelly JM, et al. Methods Mol Biol. 2012;889:25-50. doi: 10.1007/978-1-61779-867-2_4. Methods Mol Biol. 2012. PMID: 22669658
27 results