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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: kulyk s. 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: kulyk s. 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: kulyk s. 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.
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: kulyk s. 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.
Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition.
Maher JM, Zhang R, Palanisamy G, Perkins K, Liu L, Brassil P, McNamara A, Lo A, Hughes AD, Kanodia J, Kulyk S, Nikula KJ, Dengler HS, Scandurra A, Lua I, Harstad E. Maher JM, et al. Among authors: kulyk s. Toxicol Appl Pharmacol. 2022 Mar 1;438:115905. doi: 10.1016/j.taap.2022.115905. Epub 2022 Feb 3. Toxicol Appl Pharmacol. 2022. PMID: 35122773 Free article.
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