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Page 1
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers.
Smith CR, Aranda R, Bobinski TP, Briere DM, Burns AC, Christensen JG, Clarine J, Engstrom LD, Gunn RJ, Ivetac A, Jean-Baptiste R, Ketcham JM, Kobayashi M, Kuehler J, Kulyk S, Lawson JD, Moya K, Olson P, Rahbaek L, Thomas NC, Wang X, Waters LM, Marx MA. Smith CR, et al. Among authors: kuehler j. J Med Chem. 2022 Feb 10;65(3):1749-1766. doi: 10.1021/acs.jmedchem.1c01900. Epub 2022 Jan 18. J Med Chem. 2022. PMID: 35041419 Free article.
Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors.
Plewe MB, Butler SL, Dress KR, Hu Q, Johnson TW, Kuehler JE, Kuki A, Lam H, Liu W, Nowlin D, Peng Q, Rahavendran SV, Tanis SP, Tran KT, Wang H, Yang A, Zhang J. Plewe MB, et al. Among authors: kuehler je. J Med Chem. 2009 Nov 26;52(22):7211-9. doi: 10.1021/jm900862n. J Med Chem. 2009. PMID: 19873974
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Johnson TW, Tanis SP, Butler SL, Dalvie D, Delisle DM, Dress KR, Flahive EJ, Hu Q, Kuehler JE, Kuki A, Liu W, McClellan GA, Peng Q, Plewe MB, Richardson PF, Smith GL, Solowiej J, Tran KT, Wang H, Yu X, Zhang J, Zhu H. Johnson TW, et al. Among authors: kuehler je. J Med Chem. 2011 May 12;54(9):3393-417. doi: 10.1021/jm200208d. Epub 2011 Apr 13. J Med Chem. 2011. PMID: 21446745
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
Ketcham JM, Haling J, Khare S, Bowcut V, Briere DM, Burns AC, Gunn RJ, Ivetac A, Kuehler J, Kulyk S, Laguer J, Lawson JD, Moya K, Nguyen N, Rahbaek L, Saechao B, Smith CR, Sudhakar N, Thomas NC, Vegar L, Vanderpool D, Wang X, Yan L, Olson P, Christensen JG, Marx MA. Ketcham JM, et al. Among authors: kuehler j. J Med Chem. 2022 Jul 28;65(14):9678-9690. doi: 10.1021/acs.jmedchem.2c00741. Epub 2022 Jul 14. J Med Chem. 2022. PMID: 35833726 Free PMC article.
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
Smith CR, Aranda R, Christensen JG, Engstrom LD, Gunn RJ, Ivetac A, Ketcham JM, Kuehler J, David Lawson J, Marx MA, Olson P, Thomas NC, Wang X, Waters LM, Kulyk S. Smith CR, et al. Among authors: kuehler j. Bioorg Med Chem. 2022 Oct 1;71:116947. doi: 10.1016/j.bmc.2022.116947. Epub 2022 Jul 26. Bioorg Med Chem. 2022. PMID: 35926325 Free article.
Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits.
Smith CR, Kulyk S, Ahmad MUD, Arkhipova V, Christensen JG, Gunn RJ, Ivetac A, Ketcham JM, Kuehler J, Lawson JD, Thomas NC, Wang X, Marx MA. Smith CR, et al. Among authors: kuehler j. RSC Med Chem. 2022 Sep 27;13(12):1549-1564. doi: 10.1039/d2md00163b. eCollection 2022 Dec 14. RSC Med Chem. 2022. PMID: 36545438 Free PMC article.
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
Smith CR, Chen D, Christensen JG, Coulombe R, Féthière J, Gunn RJ, Hollander J, Jones B, Ketcham JM, Khare S, Kuehler J, Lawson JD, Marx MA, Olson P, Pearson KE, Ren C, Tsagris D, Ulaganathan T, Van't Veer I, Wang X, Ivetac A. Smith CR, et al. Among authors: kuehler j. J Med Chem. 2024 Jan 11;67(1):774-781. doi: 10.1021/acs.jmedchem.3c02140. Epub 2023 Dec 29. J Med Chem. 2024. PMID: 38156904 Free PMC article.
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Ketcham JM, Harwood SJ, Aranda R, Aloiau AN, Bobek BM, Briere DM, Burns AC, Caddell Haatveit K, Calinisan A, Clarine J, Elliott A, Engstrom LD, Gunn RJ, Ivetac A, Jones B, Kuehler J, Lawson JD, Nguyen N, Parker C, Pearson KE, Rahbaek L, Saechao B, Wang X, Waters A, Waters L, Watkins AH, Olson P, Smith CR, Christensen JG, Marx MA. Ketcham JM, et al. Among authors: kuehler j. J Med Chem. 2024 Mar 28;67(6):4936-4949. doi: 10.1021/acs.jmedchem.4c00078. Epub 2024 Mar 13. J Med Chem. 2024. PMID: 38477582 Free PMC article.
Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.
Tanis SP, Plewe MB, Johnson TW, Butler SL, Dalvie D, DeLisle D, Dress KR, Hu Q, Huang B, Kuehler JE, Kuki A, Liu W, Peng Q, Smith GL, Solowiej J, Tran KT, Wang H, Yang A, Yin C, Yu X, Zhang J, Zhu H. Tanis SP, et al. Among authors: kuehler je. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7429-34. doi: 10.1016/j.bmcl.2010.10.022. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036042