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Page 1
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.
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: marx ma. 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.
MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer.
Engstrom LD, Aranda R, Waters L, Moya K, Bowcut V, Vegar L, Trinh D, Hebbert A, Smith CR, Kulyk S, Lawson JD, He L, Hover LD, Fernandez-Banet J, Hallin J, Vanderpool D, Briere DM, Blaj A, Marx MA, Rodon J, Offin M, Arbour KC, Johnson ML, Kwiatkowski DJ, Jänne PA, Haddox CL, Papadopoulos KP, Henry JT, Leventakos K, Christensen JG, Shazer R, Olson P. Engstrom LD, et al. Among authors: marx ma. Cancer Discov. 2023 Nov 1;13(11):2412-2431. doi: 10.1158/2159-8290.CD-23-0669. Cancer Discov. 2023. PMID: 37552839 Free PMC article. Clinical Trial.
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: marx ma. 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: 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.
78 results