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The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Mol Cancer Ther. 2024 Apr 19. doi: 10.1158/1535-7163.MCT-23-0870. Online ahead of print.
Mol Cancer Ther. 2024.
PMID: 38641404
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: vegar l.
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.
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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: vegar l.
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.
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