Search Results - "Haling, Jacob R"

Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling by 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

“…Numerous oncogenic mutations occur within the BRAF kinase domain (BRAFKD). Here we show that stable BRAF-MEK1 complexes are enriched in BRAFWT and KRAS mutant…”
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Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers by 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

“…The mechanism of action of three different allosteric MEK inhibitors that target the MAP kinase pathway is investigated, and their efficacy is shown to be…”
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Talin-dependent integrin activation is required for fibrin clot retraction by platelets by Haling, Jacob R., Monkley, Susan J., Critchley, David R., Petrich, Brian G.

“…Talin functions both as a regulator of integrin affinity and as an important mechanical link between integrins and the cytoskeleton. Using genetic deletion of…”
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Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF by 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

“…Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709,…”
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EndoBind detects endogenous protein-protein interactions in real time by 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.

“…We present two high-throughput compatible methods to detect the interaction of ectopically expressed (RT-Bind) or endogenously tagged (EndoBind) proteins of…”
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An Experimentally Derived Database of Candidate Ras-Interacting Proteins by 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

“…We used a TAP-tag approach to identify candidate binding proteins for the related Ras family GTPases:  H-Ras, R-Ras, and Rap1A. Protein complexes were isolated…”
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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 by 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

“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology by 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

“…LONP1 is an AAA+ protease that maintains mitochondrial homeostasis by removing damaged or misfolded proteins. Elevated activity and expression of LONP1…”
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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor by 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.

“…Recent progress in targeting KRAS G12C has provided both insight and inspiration for targeting alternative KRAS mutants. In this study, we evaluated the…”
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β Integrin Tyrosine Phosphorylation Is a Conserved Mechanism for Regulating Talin-induced Integrin Activation by Anthis, Nicholas J., Haling, Jacob R., Oxley, Camilla L., Memo, Massimiliano, Wegener, Kate L., Lim, Chinten J., Ginsberg, Mark H., Campbell, Iain D.

“…Integrins are large membrane-spanning receptors fundamental to cell adhesion and migration. Integrin adhesiveness for the extracellular matrix is activated by…”
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Erratum: Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers by 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

“…Nature 501, 232–236 (2013); doi:10.1038/nature12441 In this Letter, the statement: ‘The authors declare competing financial interests: details accompany the…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers by Nishiguchi, Gisele A, Rico, Alice, Tanner, Huw, Aversa, Robert J, Taft, Benjamin R, Subramanian, Sharadha, Setti, Lina, Burger, Matthew T, Wan, Lifeng, Tamez, Victoriano, Smith, Aaron, Lou, Yan, Barsanti, Paul A, Appleton, Brent A, Mamo, Mulugeta, Tandeske, Laura, Dix, Ina, Tellew, John E, Huang, Shenlin, Mathews Griner, Lesley A, Cooke, Vesselina G, Van Abbema, Anne, Merritt, Hanne, Ma, Sylvia, Gampa, Kalyani, Feng, Fei, Yuan, Jing, Wang, Yingyun, Haling, Jacob R, Vaziri, Sepideh, Hekmat-Nejad, Mohammad, Jansen, Johanna M, Polyakov, Valery, Zang, Richard, Sethuraman, Vijay, Amiri, Payman, Singh, Mallika, Lees, Emma, Shao, Wenlin, Stuart, Darrin D, Dillon, Michael P, Ramurthy, Savithri

“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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Abstract 3499: Inhibition of SOS1 by MRTX0902 augments the anti-tumor response of the targeted EGFR inhibitor osimertinib in NSCLC by 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.

“…Abstract Osimertinib is a third generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor recommended as a first line therapy…”
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Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor by 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

“…Abstract The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at…”
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Phosphoprotein Enriched in Astrocytes 15 kDa (PEA-15) Reprograms Growth Factor Signaling by Inhibiting Threonine Phosphorylation of Fibroblast Receptor Substrate 2α by Haling, Jacob R., Wang, Fen, Ginsberg, Mark H.

“…Changes in cellular expression of phosphoprotein enriched in astrocytes of 15 kDa (PEA-15) are linked to insulin resistance, tumor cell invasion, and cellular…”
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Abstract LB-60: The BRAF:MEK complex reveals new therapeutic strategies for targeting KRASMT tumors by Haling, Jacob R., Sudhamsu, Jawahar, Hatzivassiliou, Georgia, Song, Kyung, Belvin, Marcia, Hymowitz, Sarah, Malek, Shiva

“…Abstract Spatial activation and regulation of MAPK signaling is determined by genetic context. In BRAFV600E tumor models kinase activity of BRAF is insensitive…”
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Abstract LB193: Chemical genomics identify novel druggable nodes and resistance pathways in the presence of concomitant SOS1 and KRAS inhibition by 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.

“…Abstract KRAS is the most frequently mutated oncogene in human cancer and facilitates uncontrolled growth through hyperactivation of the MAPK pathway. Recent…”
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Abstract 2346: A B-RAF-MEK complex reveals a kinase-independent role for BRAF in MAPK pathway suppression by Shiva, Malek, Haling, Jacob R., Sudhamsu, Jawahar, Morales, Tony, Peck, Ariana, Yen, Ivana, Brandhuber, Barbara, Hymowitz, Sarah

“…Abstract The Ras/RAF/MEK/ERK signaling pathway (MAPK pathway) plays a major role in growth factor-mediated cell proliferation and is frequently activated by…”
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Abstract ND02: MRTX0902: A SOS1 inhibitor for therapeutic intervention of KRAS-driven cancers by 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.

“…Abstract KRAS is the most frequently mutated oncogene in cancer and drives uncontrolled growth through hyperactivation of the MAPK pathway. Significant…”
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Anti-tumor efficacy of a potent and selective non-covalent KRAS G12D inhibitor by 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

“…Recent progress in targeting KRAS has provided both insight and inspiration for targeting alternative KRAS mutants. In this study, we evaluated the mechanism…”
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