Optimization of mTOR Inhibitors Using Property-Based Drug Design and Free-Wilson Analysis for Improved In Vivo Efficacy
Murphy, Sean T., Atienza, Joy, Brown, Jason W., Cheruvallath, Zacharia S., Cukierski, Matthew J., Fabrey, Robyn, Keung, Walter, Kwok, Lily, O'Connell, Shawn, Tang, Mingnam, Vanderpool, Darin L., Vincent, Patrick W., Zhang, Lilly, Marx, Matthew A.
Published in ACS medicinal chemistry letters (09.11.2023)
Published in ACS medicinal chemistry letters (09.11.2023)
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Journal Article
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor
Wang, Xiaolun, Allen, Shelley, Blake, James F, Bowcut, Vickie, Briere, David M, Calinisan, Andrew, Dahlke, Joshua R, Fell, Jay B, Fischer, John P, Gunn, Robin J, Hallin, Jill, Laguer, Jade, Lawson, J. David, Medwid, James, Newhouse, Brad, Nguyen, Phong, O’Leary, Jacob M, Olson, Peter, Pajk, Spencer, Rahbaek, Lisa, Rodriguez, Mareli, Smith, Christopher R, Tang, Tony P, Thomas, Nicole C, Vanderpool, Darin, Vigers, Guy P, Christensen, James G, Marx, Matthew A
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Journal Article
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 2
McBride, Christopher, Cheruvallath, Zacharia, Komandla, Mallareddy, Tang, Mingnam, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, Larson, Chris
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
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Journal Article
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction
Ketcham, John M., Haling, Jacob, Khare, Shilpi, Bowcut, Vickie, Briere, David M., Burns, Aaron C., Gunn, Robin J., Ivetac, Anthony, Kuehler, Jon, Kulyk, Svitlana, Laguer, Jade, Lawson, J. David, Moya, Krystal, Nguyen, Natalie, Rahbaek, Lisa, Saechao, Barbara, Smith, Christopher R., Sudhakar, Niranjan, Thomas, Nicole C., Vegar, Laura, Vanderpool, Darin, Wang, Xiaolun, Yan, Larry, Olson, Peter, Christensen, James G., Marx, Matthew A.
Published in Journal of medicinal chemistry (28.07.2022)
Published in Journal of medicinal chemistry (28.07.2022)
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Structure of the Human Cytomegalovirus Protease Catalytic Domain Reveals a Novel Serine Protease Fold and Catalytic Triad
Chen, Ping, Tsuge, Hideaki, Almassy, Robert J., Gribskov, Cindy L., Katoh, Susumu, Vanderpool, Darin L., Margosiak, Stephen A., Pinko, Christopher, Matthews, David A., Kan, Chen-Chen
Published in Cell (06.09.1996)
Published in Cell (06.09.1996)
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The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading
Sudhakar, Niranjan, Yan, Larry, Qiryaqos, Fadia, Engstrom, Lars D, Laguer, Jade, Calinisan, Andrew, Hebbert, Allan, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Ketcham, John M, Ivetac, Anthony, Smith, Christopher R, Lawson, J David, Rahbaek, Lisa, Clarine, Jeffrey, Nguyen, Natalie, Saechao, Barbara, Parker, Cody, Elliott, Adam J, Vanderpool, Darin, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Coma, Silvia, Pachter, Jonathan A, Hallin, Jill, Marx, Matthew A, Briere, David M, Christensen, James G, Olson, Peter, Haling, Jacob, Khare, Shilpi
Published in Molecular cancer therapeutics (01.10.2024)
Published in Molecular cancer therapeutics (01.10.2024)
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Journal Article
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading
Sudhakar, Niranjan, Yan, Larry, Qiryaqos, Fadia, Engstrom, Lars D, Laguer, Jade, Calinisan, Andrew, Hebbert, Allan, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Ketcham, John M, Ivetac, Anthony, Smith, Christopher R, Lawson, J David, Rahbaek, Lisa, Clarine, Jeffrey, Nguyen, Natalie, Saechao, Barbara, Parker, Cody, Elliott, Adam J, Vanderpool, Darin, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Coma, Silvia, Pachter, Jonathan A, Hallin, Jill, Marx, Matthew A, Briere, David M, Christensen, James G, Olson, Peter, Haling, Jacob, Khare, Shilpi
Published in Molecular cancer therapeutics (21.06.2024)
Published in Molecular cancer therapeutics (21.06.2024)
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Journal Article
MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer
Engstrom, Lars D, Aranda, Ruth, Waters, Laura, Moya, Krystal, Bowcut, Vickie, Vegar, Laura, Trinh, David, Hebbert, Allan, Smith, Christopher R, Kulyk, Svitlana, Lawson, J David, He, Leo, Hover, Laura D, Fernandez-Banet, Julio, Hallin, Jill, Vanderpool, Darin, Briere, David M, Blaj, Alice, Marx, Matthew A, Rodon, Jordi, Offin, Michael, Arbour, Kathryn C, Johnson, Melissa L, Kwiatkowski, David J, Jänne, Pasi A, Haddox, Candace L, Papadopoulos, Kyriakos P, Henry, Jason T, Leventakos, Konstantinos, Christensen, James G, Shazer, Ronald, Olson, Peter
Published in Cancer discovery (01.11.2023)
Published in Cancer discovery (01.11.2023)
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Journal Article
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
Hallin, Jill, Bowcut, Vickie, Calinisan, Andrew, Briere, David M., Hargis, Lauren, Engstrom, Lars D., Laguer, Jade, Medwid, James, Vanderpool, Darin, Lifset, Ella, Trinh, David, Hoffman, Natalie, Wang, Xiaolun, David Lawson, J., Gunn, Robin J., Smith, Christopher R., Thomas, Nicole C., Martinson, Matthew, Bergstrom, Alex, Sullivan, Francis, Bouhana, Karyn, Winski, Shannon, He, Leo, Fernandez-Banet, Julio, Pavlicek, Adam, Haling, Jacob R., Rahbaek, Lisa, Marx, Matthew A., Olson, Peter, Christensen, James G.
Published in Nature medicine (01.10.2022)
Published in Nature medicine (01.10.2022)
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Journal Article
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor
Wang, Xiaolun, Allen, Shelley, Blake, James F, Bowcut, Vickie, Briere, David M, Calinisan, Andrew, Dahlke, Joshua R, Fell, Jay B, Fischer, John P, Gunn, Robin J, Hallin, Jill, Laguer, Jade, Lawson, J David, Medwid, James, Newhouse, Brad, Nguyen, Phong, O'Leary, Jacob M, Olson, Peter, Pajk, Spencer, Rahbaek, Lisa, Rodriguez, Mareli, Smith, Christopher R, Tang, Tony P, Thomas, Nicole C, Vanderpool, Darin, Vigers, Guy P, Christensen, James G, Marx, Matthew A
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Journal Article
Abstract 3319: The MTA-cooperative PRMT5 inhibitor, MRTX1719, demonstrates increased anti-tumor activity in combination with KRAS mutant-selective inhibitors in MTAP del, KRAS -mutant cancers
Waters, Laura, Aranda, Ruth, Helu, Xousaen, Vegar, Laura, Moya, Krystal, Calinisan, Andrew, Hebbert, Allan, Hallin, Jill, Vanderpool, Darin, Briere, David M., Christensen, James G., Olson, Peter A., Engstrom, Lars D.
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
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Abstract 2778: A novel MTA-cooperative PRMT5 inhibitor, MRTX1719, stabilizes the ternary MTA-PRMT5 complex and leads to synthetic lethality in MTAP deleted cancers
Vegar, Laura, Aranda, Ruth, Waters, Laura, Moya, Krystal, Hebbert, Allan, Smith, Christopher S., Hallin, Jill, David, Briere M., Engstrom, Lars D., Vanderpool, Darin, Marx, Matthew M., Christensen, James G., Olson, Peter A.
Published in Cancer research (Chicago, Ill.) (04.04.2023)
Published in Cancer research (Chicago, Ill.) (04.04.2023)
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Abstract LB193: Chemical genomics identify novel druggable nodes and resistance pathways in the presence of concomitant SOS1 and KRAS inhibition
Khare, Shilpi, Sudhakar, Niranjan, Briere, David M., Yan, Larry, Engstrom, Lars D., Laguer, Jade, Medwid, James, Vegar, Laura, Vanderpool, Darin, Marx, Matthew A., Ketcham, John M., Christensen, James G., Olson, Peter, Haling, Jacob R.
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Journal Article
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design—Part 1
Cheruvallath, Zacharia, Tang, Mingnam, McBride, Christopher, Komandla, Mallareddy, Miura, Joanne, Ton-Nu, Thu, Erikson, Phil, Feng, Jun, Farrell, Pamela, Lawson, J. David, Vanderpool, Darin, Wu, Yiqin, Dougan, Douglas R., Plonowski, Artur, Holub, Corine, Larson, Chris
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
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Journal Article
Characterization of the CHK1 Allosteric Inhibitor Binding Site
Vanderpool, Darin, Johnson, Ted O, Ping, Chen, Bergqvist, Simon, Alton, Gordon, Phonephaly, Soneprasith, Rui, Eugene, Luo, Chun, Deng, Ya-Li, Grant, Stephan, Quenzer, Terri, Margosiak, Steve, Register, James, Brown, Ed, Ermolieff, Jacques
Published in Biochemistry (Easton) (20.10.2009)
Published in Biochemistry (Easton) (20.10.2009)
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Journal Article
Abstract ND02: MRTX0902: A SOS1 inhibitor for therapeutic intervention of KRAS-driven cancers
Ketcham, John M., Khare, Shilpi, Sudhakar, Niranjan, Briere, David M., Yan, Larry, Laguer, Jade, Vegar, Laura, Vanderpool, Darin, Hallin, Jill, Hargis, Lauren, Bowcut, Vickie, Lawson, David, Gunn, Robin J., Ivetac, Anthony, Thomas, Nicole C., Saechao, Barbara, Nguyen, Natalie, Clarine, Jeffrey, Rahbaek, Lisa, Smith, Christopher R., Burns, Aaron C., Marx, Matthew A., Christensen, James G., Olson, Peter, Haling, Jacob R.
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Abstract LB505: Design and discovery of MRTX0902, a potent, selective, and orally bioavailable SOS1 inhibitor
Ketcham, John M., Briere, David M., Burns, Aaron C., Christensen, James G., Gunn, Robin J., Haling, Jacob, Ivetac, Anthony, Khare, Shilpi, Kuehler, Jon, Kulyk, Svitlana, Laguer, Jade, Lawson, John D., Moya, Krystal, Nguyen, Natalie, Olson, Peter, Rahbaek, Lisa, Smith, Christopher R., Sudhakar, Niranjan, Thomas, Nicole C., Vanderpool, Darin, Wang, Xiaolun, Marx, Matthew A.
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Abstract 1131: Pharmacogenomic insight into targetable vulnerabilities and modifiers of response to MRTX1133 in KRASG12D-mutant models
Bowcut, Vickie, Calinisan, Andrew, Briere, David M., Hargis, Lauren, Engstrom, Lars D., Laguer, Jade, Vanderpool, Darin, Wang, Xiaolun, Lawson, J David, Thomas, Nicole, Gunn, Robin, Smith, Christopher R., Fernandez-Banet, Julio, He, Leo, Pavlicek, Adam, Rahbaek, Lisa, Marx, Matthew A., Olson, Peter, Christensen, James G., Hallin, Jill
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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