Crystal structure of human AKT1 with an allosteric inhibitor reveals a new mode of kinase inhibition von Wu, Wen-I, Voegtli, Walter C, Sturgis, Hillary L, Dizon, Faith P, Vigers, Guy P A, Brandhuber, Barbara J

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Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors von Blake, James F, Xu, Rui, Bencsik, Josef R, Xiao, Dengming, Kallan, Nicholas C, Schlachter, Stephen, Mitchell, Ian S, Spencer, Keith L, Banka, Anna L, Wallace, Eli M, Gloor, Susan L, Martinson, Matthew, Woessner, Richard D, Vigers, Guy P.A, Brandhuber, Barbara J, Liang, Jun, Safina, Brian S, Li, Jun, Zhang, Birong, Chabot, Christine, Do, Steven, Lee, Leslie, Oeh, Jason, Sampath, Deepak, Lee, Brian B, Lin, Kui, Liederer, Bianca M, Skelton, Nicholas J

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An ATP-site on-off switch that restricts phosphatase accessibility of Akt von Lin, Kui, Lin, Jie, Wu, Wen-I, Ballard, Joshua, Lee, Brian B, Gloor, Susan L, Vigers, Guy P A, Morales, Tony H, Friedman, Lori S, Skelton, Nicholas, Brandhuber, Barbara J

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Discovery and SAR of spirochromane Akt inhibitors von Kallan, Nicholas C., Spencer, Keith L., Blake, James F., Xu, Rui, Heizer, Justin, Bencsik, Josef R., Mitchell, Ian S., Gloor, Susan L., Martinson, Matthew, Risom, Tyler, Gross, Stefan D., Morales, Tony H., Wu, Wen-I, Vigers, Guy P.A., Brandhuber, Barbara J., Skelton, Nicholas J.

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Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2 von Anderson, Jake W, Vaisar, David, Jones, David N, Pegram, Laurel M, Vigers, Guy P, Chen, Huifen, Moffat, John G, Ahn, Natalie G

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RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth von Hatzivassiliou, Georgia, Song, Kyung, Yen, Ivana, Brandhuber, Barbara J., Anderson, Daniel J., Alvarado, Ryan, Ludlam, Mary J. C., Stokoe, David, Gloor, Susan L., Vigers, Guy, Morales, Tony, Aliagas, Ignacio, Liu, Bonnie, Sideris, Steve, Hoeflich, Klaus P., Jaiswal, Bijay S., Seshagiri, Somasekar, Koeppen, Hartmut, Belvin, Marcia, Friedman, Lori S., Malek, Shiva

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Multiple Active Site Corrections for Docking and Virtual Screening von Vigers, Guy P. A, Rizzi, James P

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The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients von Hallin, Jill, Engstrom, Lars D., Hargis, Lauren, Calinisan, Andrew, Aranda, Ruth, Briere, David M., Sudhakar, Niranjan, Bowcut, Vickie, Baer, Brian R., Ballard, Joshua A., Burkard, Michael R., Fell, Jay B., Fischer, John P., Vigers, Guy P., Xue, Yaohua, Gatto, Sole, Fernandez-Banet, Julio, Pavlicek, Adam, Velastagui, Karen, Chao, Richard C., Barton, Jeremy, Pierobon, Mariaelena, Baldelli, Elisa, Patricoin, Emanuel F., Cassidy, Douglas P., Marx, Matthew A., Rybkin, Igor I., Johnson, Melissa L., Ou, Sai-Hong Ignatius, Lito, Piro, Papadopoulos, Kyriakos P., Jänne, Pasi A., Olson, Peter, Christensen, James G.

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Activation loop dynamics are controlled by conformation-selective inhibitors of ERK2 von Pegram, Laurel M., Liddle, Jennifer C., Xiao, Yao, Hoh, Maria, Rudolph, Johannes, Iverson, Dylan B., Vigers, Guy P., Smith, Darin, Zhang, Hailong, Wang, Weiru, Moffat, John G., Ahn, Natalie G.

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Discovery of pyrrolopyrimidine inhibitors of Akt von Blake, James F., Kallan, Nicholas C., Xiao, Dengming, Xu, Rui, Bencsik, Josef R., Skelton, Nicholas J., Spencer, Keith L., Mitchell, Ian S., Woessner, Richard D., Gloor, Susan L., Risom, Tyler, Gross, Stefan D., Martinson, Matthew, Morales, Tony H., Vigers, Guy P.A., Brandhuber, Barbara J.

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Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors von Bencsik, Josef R., Xiao, Dengming, Blake, James F., Kallan, Nicholas C., Mitchell, Ian S., Spencer, Keith L., Xu, Rui, Gloor, Susan L., Martinson, Matthew, Risom, Tyler, Woessner, Richard D., Dizon, Faith, Wu, Wen-I, Vigers, Guy P.A., Brandhuber, Barbara J., Skelton, Nicholas J., Prior, Wei Wei, Murray, Lesley J.

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Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors von Volgraf, Matthew, Chan, Lina, Huestis, Malcolm P., Purkey, Hans E., Burkard, Michael, Geck Do, Mary, Harris, Julie, Hunt, Kevin W., Liu, Xingrong, Lyssikatos, Joseph P., Rana, Sumeet, Thomas, Allen A., Vigers, Guy P.A., Siu, Michael

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Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity von Fell, Jay B, Fischer, John P, Baer, Brian R, Ballard, Joshua, Blake, James F, Bouhana, Karyn, Brandhuber, Barbara J, Briere, David M, Burgess, Laurence E, Burkard, Michael R, Chiang, Harrah, Chicarelli, Mark J, Davidson, Kevin, Gaudino, John J, Hallin, Jill, Hanson, Lauren, Hee, Kenneth, Hicken, Erik J, Hinklin, Ronald J, Marx, Matthew A, Mejia, Macedonio J, Olson, Peter, Savechenkov, Pavel, Sudhakar, Niranjan, Tang, Tony P, Vigers, Guy P, Zecca, Henry, Christensen, James G

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor von 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

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Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA von Xu, Rui, Banka, Anna, Blake, James F., Mitchell, Ian S., Wallace, Eli M., Bencsik, Josef R., Kallan, Nicholas C., Spencer, Keith L., Gloor, Susan L., Martinson, Matthew, Risom, Tyler, Gross, Stefan D., Morales, Tony H., Wu, Wen-I, Vigers, Guy P.A., Brandhuber, Barbara J., Skelton, Nicholas J.

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Identification of the Clinical Development Candidate MRTX849 , a Covalent KRAS G12C Inhibitor for the Treatment of Cancer von 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, Marx, Matthew A

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Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor von 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

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Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer von 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, Marx, Matthew A

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Crystal structure of the type-I interleukin-1 receptor complexed with interleukin-1β von Vigers, Guy P. A., Anderson, Lana J., Caffes, Patricia, Brandhuber, Barbara J.

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X-ray Crystal Structure of a Small Antagonist Peptide Bound to Interleukin-1 Receptor Type 1 von Vigers, Guy P.A., Dripps, David J., Edwards, Carl K., Brandhuber, Barbara J.

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