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Page 1
Optimization of mTOR Inhibitors Using Property-Based Drug Design and Free-Wilson Analysis for Improved In Vivo Efficacy.
Murphy ST, Atienza J, Brown JW, Cheruvallath ZS, Cukierski MJ, Fabrey R, Keung W, Kwok L, O'Connell S, Tang M, Vanderpool DL, Vincent PW, Zhang L, Marx MA. Murphy ST, et al. Among authors: vanderpool dl. ACS Med Chem Lett. 2023 Oct 25;14(11):1544-1550. doi: 10.1021/acsmedchemlett.3c00351. eCollection 2023 Nov 9. ACS Med Chem Lett. 2023. PMID: 37970587 Free PMC article.
Characterization of the CHK1 allosteric inhibitor binding site.
Vanderpool D, Johnson TO, Ping C, Bergqvist S, Alton G, Phonephaly S, Rui E, Luo C, Deng YL, Grant S, Quenzer T, Margosiak S, Register J, Brown E, Ermolieff J. Vanderpool D, et al. Biochemistry. 2009 Oct 20;48(41):9823-30. doi: 10.1021/bi900258v. Biochemistry. 2009. PMID: 19743875
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 1.
Cheruvallath Z, Tang M, McBride C, Komandla M, Miura J, Ton-Nu T, Erikson P, Feng J, Farrell P, Lawson JD, Vanderpool D, Wu Y, Dougan DR, Plonowski A, Holub C, Larson C. Cheruvallath Z, et al. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2774-2778. doi: 10.1016/j.bmcl.2016.04.073. Epub 2016 Apr 25. Bioorg Med Chem Lett. 2016. PMID: 27155900
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. 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.
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. 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.
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Sudhakar N, Yan L, Qiryaqos F, Engstrom LD, Laguer J, Calinisan A, Hebbert A, Waters L, Moya K, Bowcut V, Vegar L, Ketcham JM, Ivetac A, Smith CR, Lawson JD, Rahbaek L, Clarine J, Nguyen N, Saechao B, Parker C, Elliott AJ, Vanderpool D, He L, Hover LD, Fernandez-Banet J, Coma S, Pachter JA, Hallin J, Marx MA, Briere DM, Christensen JG, Olson P, Haling J, Khare S. Sudhakar N, et al. Mol Cancer Ther. 2024 Apr 19. doi: 10.1158/1535-7163.MCT-23-0870. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38641404
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor.
Hallin J, Bowcut V, Calinisan A, Briere DM, Hargis L, Engstrom LD, Laguer J, Medwid J, Vanderpool D, Lifset E, Trinh D, Hoffman N, Wang X, David Lawson J, Gunn RJ, Smith CR, Thomas NC, Martinson M, Bergstrom A, Sullivan F, Bouhana K, Winski S, He L, Fernandez-Banet J, Pavlicek A, Haling JR, Rahbaek L, Marx MA, Olson P, Christensen JG. Hallin J, et al. Nat Med. 2022 Oct;28(10):2171-2182. doi: 10.1038/s41591-022-02007-7. Epub 2022 Oct 10. Nat Med. 2022. PMID: 36216931
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. 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.
15 results