Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling
Haling, Jacob R., Sudhamsu, Jawahar, Yen, Ivana, Sideris, Steve, Sandoval, Wendy, Phung, Wilson, Bravo, Brandon J., Giannetti, Anthony M., Peck, Ariana, Masselot, Alexandre, Morales, Tony, Smith, Darin, Brandhuber, Barbara J., Hymowitz, Sarah G., Malek, Shiva
Published in Cancer cell (08.09.2014)
Published in Cancer cell (08.09.2014)
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Journal Article
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, Georgia, Haling, Jacob R., Chen, Huifen, Song, Kyung, Price, Steve, Heald, Robert, Hewitt, Joanne F. M., Zak, Mark, Peck, Ariana, Orr, Christine, Merchant, Mark, Hoeflich, Klaus P., Chan, Jocelyn, Luoh, Shiuh-Ming, Anderson, Daniel J., Ludlam, Mary J. C., Wiesmann, Christian, Ultsch, Mark, Friedman, Lori S., Malek, Shiva, Belvin, Marcia
Published in Nature (London) (12.09.2013)
Published in Nature (London) (12.09.2013)
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Journal Article
Talin-dependent integrin activation is required for fibrin clot retraction by platelets
Haling, Jacob R., Monkley, Susan J., Critchley, David R., Petrich, Brian G.
Published in Blood (03.02.2011)
Published in Blood (03.02.2011)
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Journal Article
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF
Shao, Wenlin, Mishina, Yuji M, Feng, Yun, Caponigro, Giordano, Cooke, Vesselina G, Rivera, Stacy, Wang, Yingyun, Shen, Fang, Korn, Joshua M, Mathews Griner, Lesley A, Nishiguchi, Gisele, Rico, Alice, Tellew, John, Haling, Jacob R, Aversa, Robert, Polyakov, Valery, Zang, Richard, Hekmat-Nejad, Mohammad, Amiri, Payman, Singh, Mallika, Keen, Nicholas, Dillon, Michael P, Lees, Emma, Ramurthy, Savithri, Sellers, William R, Stuart, Darrin D
Published in Cancer research (Chicago, Ill.) (15.03.2018)
Published in Cancer research (Chicago, Ill.) (15.03.2018)
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Journal Article
Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Ramurthy, Savithri, Taft, Benjamin R, Aversa, Robert J, Barsanti, Paul A, Burger, Matthew T, Lou, Yan, Nishiguchi, Gisele A, Rico, Alice, Setti, Lina, Smith, Aaron, Subramanian, Sharadha, Tamez, Victoriano, Tanner, Huw, Wan, Lifeng, Hu, Cheng, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Tellew, John E, Huang, Shenlin, Yue, Qin, Chaudhary, Apurva, Tian, Hung, Iyer, Raman, Hassan, A. Quamrul, Mathews Griner, Lesley A, La Bonte, Laura R, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Mishina, Yuji, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Sellers, William R, Lees, Emma, Shao, Wenlin, Dillon, Michael P, Stuart, Darrin D
Published in Journal of medicinal chemistry (12.03.2020)
Published in Journal of medicinal chemistry (12.03.2020)
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Journal Article
Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology
Kingsley, Laura J, He, Xiaohui, McNeill, Matthew, Nelson, John, Nikulin, Victor, Ma, Zhiwei, Lu, Wenshuo, Zhou, Vicki W, Manuia, Mari, Kreusch, Andreas, Gao, Mu-Yun, Witmer, Darbi, Vaillancourt, Mei-Ting, Lu, Min, Greenblatt, Sarah, Lee, Christian, Vashisht, Ajay, Bender, Steven, Spraggon, Glen, Michellys, Pierre-Yves, Jia, Yong, Haling, Jacob R, Lelais, Gérald
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
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Journal Article
BRAF-inhibitor Associated MEK Mutations Increase RAF-Dependent and -Independent Enzymatic Activity
Emery, Caroline M, Monaco, Kelli-Ann, Wang, Ping, Balak, Marissa, Freeman, Alyson, Meltzer, Jodi, Delach, Scott M, Rakiec, Daniel, Ruddy, David A, Korn, Joshua M, Haling, Jacob, Acker, Michael G, Caponigro, Giordano
Published in Molecular cancer research (01.10.2017)
Published in Molecular cancer research (01.10.2017)
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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
β Integrin Tyrosine Phosphorylation Is a Conserved Mechanism for Regulating Talin-induced Integrin Activation
Anthis, Nicholas J., Haling, Jacob R., Oxley, Camilla L., Memo, Massimiliano, Wegener, Kate L., Lim, Chinten J., Ginsberg, Mark H., Campbell, Iain D.
Published in The Journal of biological chemistry (25.12.2009)
Published in The Journal of biological chemistry (25.12.2009)
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Journal Article
Abl-interactor-1 (Abi1) has a role in cardiovascular and placental development and is a binding partner of the α4 integrin
Ring, Colleen, Ginsberg, Mark H, Haling, Jacob, Pendergast, Ann Marie
Published in Proceedings of the National Academy of Sciences - PNAS (04.01.2011)
Published in Proceedings of the National Academy of Sciences - PNAS (04.01.2011)
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Journal Article
EndoBind detects endogenous protein-protein interactions in real time
Bill, Anke, Espinola, Sheryll, Guthy, Daniel, Haling, Jacob R., Lanter, Mylene, Lu, Min, Marelli, Anthony, Mendiola, Angelica, Miraglia, Loren, Taylor, Brandon L., Vargas, Leonardo, Orth, Anthony P., King, Frederick J.
Published in Communications biology (15.09.2021)
Published in Communications biology (15.09.2021)
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Journal Article
An Experimentally Derived Database of Candidate Ras-Interacting Proteins
Goldfinger, Lawrence E, Ptak, Celeste, Jeffery, Erin D, Shabanowitz, Jeffrey, Han, Jaewon, Haling, Jacob R, Sherman, Nicholas E, Fox, Jay W, Hunt, Donald F, Ginsberg, Mark H
Published in Journal of proteome research (01.05.2007)
Published in Journal of proteome research (01.05.2007)
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Journal Article
Erratum: Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, Georgia, Haling, Jacob R., Chen, Huifen, Song, Kyung, Price, Steve, Heald, Robert, Hewitt, Joanne F. M., Zak, Mark, Peck, Ariana, Orr, Christine, Merchant, Mark, Hoeflich, Klaus P., Chan, Jocelyn, Luoh, Shiuh-Ming, Anderson, Daniel J., Ludlam, Mary J. C., Wiesmann, Christian, Ultsch, Mark, Friedman, Lori S., Malek, Shiva, Belvin, Marcia
Published in Nature (London) (10.10.2013)
Published in Nature (London) (10.10.2013)
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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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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 (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
Abstract 3499: Inhibition of SOS1 by MRTX0902 augments the anti-tumor response of the targeted EGFR inhibitor osimertinib in NSCLC
Khare, Shilpi, Sudhakar, Niranjan, Laguer, Jade, Briere, David M., Yan, Larry, Hebbert, Allan, Calinisan, Andrew, Engstrom, Lars D., Qiryaqos, Fadia, Olson, Peter, Christensen, James G., Haling, Jacob R.
Published in Cancer research (Chicago, Ill.) (04.04.2023)
Published in Cancer research (Chicago, Ill.) (04.04.2023)
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Journal Article
Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor
Stuart, Darrin D., Shao, Wenlin, Mishina, Yuji, Feng, Yun, Caponigro, Giordano, Cooke, Vesselina G., Rivera, Stacey, Shen, Fang, Korn, Joshua, Griner, Lesley A. Mathews, Nishiguchi, Giselle, Taft, Benjamin, Wan, Lifeng, Subramanian, Sharadha, Lou, Yan, Setti, Lina, Burger, Matthew, Tamez, Victor, Rico, Alice, Aversa, Robert, Tellew, John, Haling, Jacob R., Polyakov, Valery, Lambert, Amy, Zang, Richard, Abbema, Ann Van, Hekmat-Nejad, Mohamad, Amiri, Payman, Singh, Mallika, Keen, Nicholas, Dillon, Michael P., Lees, Emma, Sellers, William R., Ramurthy, Savithri
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Journal Article
Abstract LB-60: The BRAF:MEK complex reveals new therapeutic strategies for targeting KRASMT tumors
Haling, Jacob R., Sudhamsu, Jawahar, Hatzivassiliou, Georgia, Song, Kyung, Belvin, Marcia, Hymowitz, Sarah, Malek, Shiva
Published in Cancer research (Chicago, Ill.) (15.04.2013)
Published in Cancer research (Chicago, Ill.) (15.04.2013)
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