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10 results on '"Olson, Peter"'

1. Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein

Author

Ketcham, John M., primary, Harwood, Stephen J., additional, Aranda, Ruth, additional, Aloiau, Athenea N., additional, Bobek, Briana M., additional, Briere, David M., additional, Burns, Aaron C., additional, Caddell Haatveit, Kersti, additional, Calinisan, Andrew, additional, Clarine, Jeffery, additional, Elliott, Adam, additional, Engstrom, Lars D., additional, Gunn, Robin J., additional, Ivetac, Anthony, additional, Jones, Benjamin, additional, Kuehler, Jon, additional, Lawson, J. David, additional, Nguyen, Natalie, additional, Parker, Cody, additional, Pearson, Kelly E., additional, Rahbaek, Lisa, additional, Saechao, Barbara, additional, Wang, Xiaolun, additional, Waters, Anna, additional, Waters, Laura, additional, Watkins, Ashlee H., additional, Olson, Peter, additional, Smith, Christopher R., additional, Christensen, James G., additional, and Marx, Matthew A., additional

Published
2024
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2. Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X‑Ray Cocrystallography.

Author

Smith, Christopher R., Chen, Dan, Christensen, James G., Coulombe, René, Féthière, James, Gunn, Robin J., Hollander, Johan, Jones, Benjamin, Ketcham, John M., Khare, Shilpi, Kuehler, Jon, Lawson, J. David, Marx, Matthew A., Olson, Peter, Pearson, Kelly E., Ren, Cynthia, Tsagris, Denise, Ulaganathan, Thirumalaiselvi, Van't Veer, Inge, and Wang, Xiaolun

Published
2024
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3. Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction

Author

Ketcham, John M., primary, Haling, Jacob, additional, Khare, Shilpi, additional, Bowcut, Vickie, additional, Briere, David M., additional, Burns, Aaron C., additional, Gunn, Robin J., additional, Ivetac, Anthony, additional, Kuehler, Jon, additional, Kulyk, Svitlana, additional, Laguer, Jade, additional, Lawson, J. David, additional, Moya, Krystal, additional, Nguyen, Natalie, additional, Rahbaek, Lisa, additional, Saechao, Barbara, additional, Smith, Christopher R., additional, Sudhakar, Niranjan, additional, Thomas, Nicole C., additional, Vegar, Laura, additional, Vanderpool, Darin, additional, Wang, Xiaolun, additional, Yan, Larry, additional, Olson, Peter, additional, Christensen, James G., additional, and Marx, Matthew A., additional

Published
2022
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4. Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers

Author

Smith, Christopher R., primary, Aranda, Ruth, additional, Bobinski, Thomas P., additional, Briere, David M., additional, Burns, Aaron C., additional, Christensen, James G., additional, Clarine, Jeffery, additional, Engstrom, Lars D., additional, Gunn, Robin J., additional, Ivetac, Anthony, additional, Jean-Baptiste, Ronald, additional, Ketcham, John M., additional, Kobayashi, Masakazu, additional, Kuehler, Jon, additional, Kulyk, Svitlana, additional, Lawson, J. David, additional, Moya, Krystal, additional, Olson, Peter, additional, Rahbaek, Lisa, additional, Thomas, Nicole C., additional, Wang, Xiaolun, additional, Waters, Laura M., additional, and Marx, Matthew A., additional

Published
2022
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5. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

Author

Wang, Xiaolun, primary, Allen, Shelley, additional, Blake, James F., additional, Bowcut, Vickie, additional, Briere, David M., additional, Calinisan, Andrew, additional, Dahlke, Joshua R., additional, Fell, Jay B., additional, Fischer, John P., additional, Gunn, Robin J., additional, Hallin, Jill, additional, Laguer, Jade, additional, Lawson, J. David, additional, Medwid, James, additional, Newhouse, Brad, additional, Nguyen, Phong, additional, O’Leary, Jacob M., additional, Olson, Peter, additional, Pajk, Spencer, additional, Rahbaek, Lisa, additional, Rodriguez, Mareli, additional, Smith, Christopher R., additional, Tang, Tony P., additional, Thomas, Nicole C., additional, Vanderpool, Darin, additional, Vigers, Guy P., additional, Christensen, James G., additional, and Marx, Matthew A., additional

Published
2021
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6. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

Author

Fell, Jay B., primary, Fischer, John P., additional, Baer, Brian R., additional, Blake, James F., additional, Bouhana, Karyn, additional, Briere, David M., additional, Brown, Karin D., additional, Burgess, Laurence E., additional, Burns, Aaron C., additional, Burkard, Michael R., additional, Chiang, Harrah, additional, Chicarelli, Mark J., additional, Cook, Adam W., additional, Gaudino, John J., additional, Hallin, Jill, additional, Hanson, Lauren, additional, Hartley, Dylan P., additional, Hicken, Erik J., additional, Hingorani, Gary P., additional, Hinklin, Ronald J., additional, Mejia, Macedonio J., additional, Olson, Peter, additional, Otten, Jennifer N., additional, Rhodes, Susan P., additional, Rodriguez, Martha E., additional, Savechenkov, Pavel, additional, Smith, Darin J., additional, Sudhakar, Niranjan, additional, Sullivan, Francis X., additional, Tang, Tony P., additional, Vigers, Guy P., additional, Wollenberg, Lance, additional, Christensen, James G., additional, and Marx, Matthew A., additional

Published
2020
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8. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12CInhibitor for the Treatment of Cancer

Author

Fell, Jay B., Fischer, John P., Baer, Brian R., Blake, James F., Bouhana, Karyn, Briere, David M., Brown, Karin D., Burgess, Laurence E., Burns, Aaron C., Burkard, Michael R., Chiang, Harrah, Chicarelli, Mark J., Cook, Adam W., Gaudino, John J., Hallin, Jill, Hanson, Lauren, Hartley, Dylan P., Hicken, Erik J., Hingorani, Gary P., Hinklin, Ronald J., Mejia, Macedonio J., Olson, Peter, Otten, Jennifer N., Rhodes, Susan P., Rodriguez, Martha E., Savechenkov, Pavel, Smith, Darin J., Sudhakar, Niranjan, Sullivan, Francis X., Tang, Tony P., Vigers, Guy P., Wollenberg, Lance, Christensen, James G., and Marx, Matthew A.

Abstract

Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target’s resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRASG12Cthat bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogues were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clinical development candidate MRTX849as a potent, selective covalent inhibitor of KRASG12Cis described.

Published
2020
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9. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor.

Author

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, and Marx MA

Subjects
Animals, Antineoplastic Agents chemistry, Drug Discovery, Humans, Mice, Models, Molecular, Mutation, Proto-Oncogene Proteins p21(ras) genetics, Structure-Activity Relationship, Xenograft Model Antitumor Assays, Antineoplastic Agents pharmacology, Proto-Oncogene Proteins p21(ras) antagonists & inhibitors
Abstract

KRAS G12D , the most common oncogenic KRAS mutation, is a promising target for the treatment of solid tumors. However, when compared to KRAS G12C , selective inhibition of KRAS G12D presents a significant challenge due to the requirement of inhibitors to bind KRAS G12D with high enough affinity to obviate the need for covalent interactions with the mutant KRAS protein. Here, we report the discovery and characterization of the first noncovalent, potent, and selective KRAS G12D inhibitor, MRTX1133, which was discovered through an extensive structure-based activity improvement and shown to be efficacious in a KRAS G12D mutant xenograft mouse tumor model.

Published
2022
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10. Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer.

Author

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, and Marx MA

Subjects
Animals, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacokinetics, Cell Line, Tumor, Drug Design, Drug Screening Assays, Antitumor, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacokinetics, Humans, Mice, Models, Molecular, Mutation, Proto-Oncogene Proteins p21(ras) chemistry, Proto-Oncogene Proteins p21(ras) genetics, Xenograft Model Antitumor Assays, Antineoplastic Agents pharmacology, Enzyme Inhibitors pharmacology, Proto-Oncogene Proteins p21(ras) antagonists & inhibitors
Abstract

Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRAS G12C that bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogues were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRAS G12C is described.

Published
2020
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