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Page 1
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: marx ma. 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.
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH. Murphy ST, et al. Among authors: marx ma. J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22040023
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. Cheng H, et al. Among authors: marx ma. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. doi: 10.1021/ml300309h. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900568 Free PMC article.
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG. Fell JB, et al. Among authors: marx ma. ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613331 Free PMC article.
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue Y, Gatto S, Fernandez-Banet J, Pavlicek A, Velastagui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF 3rd, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Jänne PA, Olson P, Christensen JG. Hallin J, et al. Among authors: marx ma. Cancer Discov. 2020 Jan;10(1):54-71. doi: 10.1158/2159-8290.CD-19-1167. Epub 2019 Oct 28. Cancer Discov. 2020. PMID: 31658955 Free PMC article.
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
Fell JB, Fischer JP, Baer BR, Blake JF, Bouhana K, Briere DM, Brown KD, Burgess LE, Burns AC, Burkard MR, Chiang H, Chicarelli MJ, Cook AW, Gaudino JJ, Hallin J, Hanson L, Hartley DP, Hicken EJ, Hingorani GP, Hinklin RJ, Mejia MJ, Olson P, Otten JN, Rhodes SP, Rodriguez ME, Savechenkov P, Smith DJ, Sudhakar N, Sullivan FX, Tang TP, Vigers GP, Wollenberg L, Christensen JG, Marx MA. Fell JB, et al. Among authors: marx ma. J Med Chem. 2020 Jul 9;63(13):6679-6693. doi: 10.1021/acs.jmedchem.9b02052. Epub 2020 Apr 6. J Med Chem. 2020. PMID: 32250617 Free article.
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor.
Wang X, Allen S, Blake JF, Bowcut V, Briere DM, Calinisan A, Dahlke JR, Fell JB, Fischer JP, Gunn RJ, Hallin J, Laguer J, Lawson JD, Medwid J, Newhouse B, Nguyen P, O'Leary JM, Olson P, Pajk S, Rahbaek L, Rodriguez M, Smith CR, Tang TP, Thomas NC, Vanderpool D, Vigers GP, Christensen JG, Marx MA. Wang X, et al. Among authors: marx ma. J Med Chem. 2022 Feb 24;65(4):3123-3133. doi: 10.1021/acs.jmedchem.1c01688. Epub 2021 Dec 10. J Med Chem. 2022. PMID: 34889605 Free article.
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: marx ma. 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.
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: marx ma. 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: marx ma. 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.
79 results