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

Volltext

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

Volltext

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

Volltext

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

Volltext

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

Volltext

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.

Volltext

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.

Volltext

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

Volltext

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

Volltext

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.

Volltext

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.

Volltext

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.

Volltext

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.

Volltext

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

Volltext

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

Volltext

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.

Volltext

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

Volltext

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

Volltext

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

Volltext

Abstract B30: Structure-based drug discovery of MRTX1257, a selective, covalent KRAS G12C inhibitor with oral activity in animal models of cancer von Marx, Matthew A., Baer, Brian R., Ballard, Joshua, Blake, James F., Bouhana, Karyn, Briere, David M., Burgess, Laurence E., Burkhard, Michael R., Chiang, Harrah, Chicarelli, Mark J., Christensen, James G., Fischer, John P., Hallin, Jill, Mejia, Macedonia J., Olson, Peter, Savechenkov, Pavel, Sudhakar, Niranjan, Tang, Tony P., Vigers, Guy P., Fell, Jay B.

Volltext