Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer von Jin, Lingyan, Garcia, Jesse, Chan, Emily, de la Cruz, Cecile, Segal, Ehud, Merchant, Mark, Kharbanda, Samir, Raisner, Ryan, Haverty, Peter M, Modrusan, Zora, Ly, Justin, Choo, Edna, Kaufman, Susan, Beresini, Maureen H, Romero, F Anthony, Magnuson, Steven, Gascoigne, Karen E

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Structural basis for dual-mode inhibition of the ABC transporter MsbA von Ho, Hoangdung, Miu, Anh, Alexander, Mary Kate, Garcia, Natalie K., Oh, Angela, Zilberleyb, Inna, Reichelt, Mike, Austin, Cary D., Tam, Christine, Shriver, Stephanie, Hu, Huiyong, Labadie, Sharada S., Liang, Jun, Wang, Lan, Wang, Jian, Lu, Yan, Purkey, Hans E., Quinn, John, Franke, Yvonne, Clark, Kevin, Beresini, Maureen H., Tan, Man-Wah, Sellers, Benjamin D., Maurer, Till, Koehler, Michael F. T., Wecksler, Aaron T., Kiefer, James R., Verma, Vishal, Xu, Yiming, Nishiyama, Mireille, Payandeh, Jian, Koth, Christopher M.

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USP7 small-molecule inhibitors interfere with ubiquitin binding von Kategaya, Lorna, Di Lello, Paola, Rougé, Lionel, Pastor, Richard, Clark, Kevin R., Drummond, Jason, Kleinheinz, Tracy, Lin, Eva, Upton, John-Paul, Prakash, Sumit, Heideker, Johanna, McCleland, Mark, Ritorto, Maria Stella, Alessi, Dario R., Trost, Matthias, Bainbridge, Travis W., Kwok, Michael C. M., Ma, Taylur P., Stiffler, Zachary, Brasher, Bradley, Tang, Yinyan, Jaishankar, Priyadarshini, Hearn, Brian R., Renslo, Adam R., Arkin, Michelle R., Cohen, Frederick, Yu, Kebing, Peale, Frank, Gnad, Florian, Chang, Matthew T., Klijn, Christiaan, Blackwood, Elizabeth, Martin, Scott E., Forrest, William F., Ernst, James A., Ndubaku, Chudi, Wang, Xiaojing, Beresini, Maureen H., Tsui, Vickie, Schwerdtfeger, Carsten, Blake, Robert A., Murray, Jeremy, Maurer, Till, Wertz, Ingrid E.

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Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists von Zhang, Yingnan, Ultsch, Mark, Skelton, Nicholas J, Burdick, Daniel J, Beresini, Maureen H, Li, Wei, Kong-Beltran, Monica, Peterson, Andrew, Quinn, John, Chiu, Cecilia, Wu, Yan, Shia, Steven, Moran, Paul, Di Lello, Paola, Eigenbrot, Charles, Kirchhofer, Daniel

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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300 von Crawford, Terry D, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Taylor, Alexander M, de Leon Boenig, Gladys, Noland, Cameron L, Murray, Jeremy, Ly, Justin, Choo, Edna F, Hunsaker, Thomas L, Chan, Emily W, Merchant, Mark, Kharbanda, Samir, Gascoigne, Karen E, Kaufman, Susan, Beresini, Maureen H, Liao, Jiangpeng, Liu, Wenfeng, Chen, Kevin X, Chen, Zhongguo, Conery, Andrew R, Côté, Alexandre, Jayaram, Hariharan, Jiang, Ying, Kiefer, James R, Kleinheinz, Tracy, Li, Yingjie, Maher, Jonathan, Pardo, Eneida, Poy, Florence, Spillane, Kerry L, Wang, Fei, Wang, Jian, Wei, Xiaocang, Xu, Zhaowu, Xu, Zhongya, Yen, Ivana, Zawadzke, Laura, Zhu, Xiaoyu, Bellon, Steven, Cummings, Richard, Cochran, Andrea G, Albrecht, Brian K, Magnuson, Steven

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Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands von Ferri, Elena, Le Thomas, Adrien, Wallweber, Heidi Ackerly, Day, Eric S., Walters, Benjamin T., Kaufman, Susan E., Braun, Marie-Gabrielle, Clark, Kevin R., Beresini, Maureen H., Mortara, Kyle, Chen, Yung-Chia A., Canter, Breanna, Phung, Wilson, Liu, Peter S., Lammens, Alfred, Ashkenazi, Avi, Rudolph, Joachim, Wang, Weiru

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Disruption of IRE1α through its kinase domain attenuates multiple myeloma von Harnoss, Jonathan M., Le Thomas, Adrien, Shemorry, Anna, Marsters, Scot A., Lawrence, David A., Lu, Min, Chen, Yung-Chia Ariel, Qing, Jing, Totpal, Klara, Kan, David, Segal, Ehud, Merchant, Mark, Reichelt, Mike, Wallweber, Heidi Ackerly, Wang, Weiru, Clark, Kevin, Kaufman, Susan, Beresini, Maureen H., Laing, Steven T., Sandoval, Wendy, Lorenzo, Maria, Wu, Jiansheng, Ly, Justin, De Bruyn, Tom, Heidersbach, Amy, Haley, Benjamin, Gogineni, Alvin, Weimer, Robby M., Lee, Dong, Braun, Marie-Gabrielle, Rudolph, Joachim, VanWyngarden, Michael J., Sherbenou, Daniel W., Gomez-Bougie, Patricia, Amiot, Martine, Acosta-Alvear, Diego, Walter, Peter, Ashkenazi, Avi

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High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRASG12C by Intact Protein MS and Targeted MRM von Li, Ke Sherry, Quinn, John G, Saabye, Matthew J, Guerrero, Jesus F. Salcido, Nonomiya, Jim, Lian, Qihui, Phung, Wilson, Izrayelit, Yevgeniy, Walters, Benjamin T, Gustafson, Amy, Endres, Nicholas F, Beresini, Maureen H, Mulvihill, Melinda M

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GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) von Romero, F. Anthony, Murray, Jeremy, Lai, Kwong Wah, Tsui, Vickie, Albrecht, Brian K, An, Le, Beresini, Maureen H, de Leon Boenig, Gladys, Bronner, Sarah M, Chan, Emily W, Chen, Kevin X, Chen, Zhongguo, Choo, Edna F, Clagg, Kyle, Clark, Kevin, Crawford, Terry D, Cyr, Patrick, de Almeida Nagata, Denise, Gascoigne, Karen E, Grogan, Jane L, Hatzivassiliou, Georgia, Huang, Wei, Hunsaker, Thomas L, Kaufman, Susan, Koenig, Stefan G, Li, Ruina, Li, Yingjie, Liang, Xiaorong, Liao, Jiangpeng, Liu, Wenfeng, Ly, Justin, Maher, Jonathan, Masui, Colin, Merchant, Mark, Ran, Yingqing, Taylor, Alexander M, Wai, John, Wang, Fei, Wei, Xiaocang, Yu, Dong, Zhu, Bing-Yan, Zhu, Xiaoyu, Magnuson, Steven

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Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model von Braun, Marie-Gabrielle, Ashkenazi, Avi, Beveridge, Ramsay E., Castanedo, Georgette, Wallweber, Heidi Ackerly, Beresini, Maureen H., Clark, Kevin R., De Bruyn, Tom, Fu, Liqiang, Gibbons, Paul, Jiang, Fan, Kaufman, Susan, Kan, David, Kiefer, James R., Leclerc, Jean-Philippe, Lemire, Alexandre, Ly, Cuong, Segal, Ehud, Sims, Jessica, Wang, Weiru, Wei, Wentao, Zhao, Liang, Schwarz, Jacob B., Rudolph, Joachim

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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains von Crawford, Terry D, Tsui, Vickie, Flynn, E. Megan, Wang, Shumei, Taylor, Alexander M, Côté, Alexandre, Audia, James E, Beresini, Maureen H, Burdick, Daniel J, Cummings, Richard, Dakin, Les A, Duplessis, Martin, Good, Andrew C, Hewitt, Michael C, Huang, Hon-Ren, Jayaram, Hariharan, Kiefer, James R, Jiang, Ying, Murray, Jeremy, Nasveschuk, Christopher G, Pardo, Eneida, Poy, Florence, Romero, F. Anthony, Tang, Yong, Wang, Jian, Xu, Zhaowu, Zawadzke, Laura E, Zhu, Xiaoyu, Albrecht, Brian K, Magnuson, Steven R, Bellon, Steve, Cochran, Andrea G

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Design of Organo-Peptides As Bipartite PCSK9 Antagonists von Burdick, Daniel J, Skelton, Nicholas J, Ultsch, Mark, Beresini, Maureen H, Eigenbrot, Charles, Li, Wei, Zhang, Yingnan, Nguyen, Huy, Kong-Beltran, Monica, Quinn, John G, Kirchhofer, Daniel

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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637) von Taylor, Alexander M, Côté, Alexandre, Hewitt, Michael C, Pastor, Richard, Leblanc, Yves, Nasveschuk, Christopher G, Romero, F. Anthony, Crawford, Terry D, Cantone, Nico, Jayaram, Hariharan, Setser, Jeremy, Murray, Jeremy, Beresini, Maureen H, de Leon Boenig, Gladys, Chen, Zhongguo, Conery, Andrew R, Cummings, Richard T, Dakin, Leslie A, Flynn, E. Megan, Huang, Oscar W, Kaufman, Susan, Keller, Patricia J, Kiefer, James R, Lai, Tommy, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Lu, Henry, Pardo, Eneida, Tsui, Vickie, Wang, Jian, Wang, Yongyun, Xu, Zhaowu, Yan, Fen, Yu, Dong, Zawadzke, Laura, Zhu, Xiaoqin, Zhu, Xiaoyu, Sims, Robert J, Cochran, Andrea G, Bellon, Steve, Audia, James E, Magnuson, Steven, Albrecht, Brian K

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Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152) von Flygare, John A, Beresini, Maureen, Budha, Nageshwar, Chan, Helen, Chan, Iris T, Cheeti, Sravanthi, Cohen, Frederick, Deshayes, Kurt, Doerner, Karl, Eckhardt, S. Gail, Elliott, Linda O, Feng, Bainian, Franklin, Matthew C, Reisner, Stacy Frankovitz, Gazzard, Lewis, Halladay, Jason, Hymowitz, Sarah G, La, Hank, LoRusso, Patricia, Maurer, Brigitte, Murray, Lesley, Plise, Emile, Quan, Clifford, Stephan, Jean-Philippe, Young, Shin G, Tom, Jeffrey, Tsui, Vickie, Um, Joanne, Varfolomeev, Eugene, Vucic, Domagoj, Wagner, Andrew J, Wallweber, Heidi J. A, Wang, Lan, Ware, Joseph, Wen, Zhaoyang, Wong, Harvey, Wong, Jonathan M, Wong, Melisa, Wong, Susan, Yu, Ron, Zobel, Kerry, Fairbrother, Wayne J

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High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRAS G12C by Intact Protein MS and Targeted MRM von Li, Ke Sherry, Quinn, John G, Saabye, Matthew J, Guerrero, Jesus F Salcido, Nonomiya, Jim, Lian, Qihui, Phung, Wilson, Izrayelit, Yevgeniy, Walters, Benjamin T, Gustafson, Amy, Endres, Nicholas F, Beresini, Maureen H, Mulvihill, Melinda M

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A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors von Bronner, Sarah M, Murray, Jeremy, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Cyr, Patrick, Beresini, Maureen H, de leon Boenig, Gladys, Chen, Zhongguo, Choo, Edna F, Clark, Kevin R, Crawford, Terry D, Jayaram, Hariharan, Kaufman, Susan, Li, Ruina, Li, Yingjie, Liao, Jiangpeng, Liang, Xiaorong, Liu, Wenfeng, Ly, Justin, Maher, Jonathan, Wai, John, Wang, Fei, Zheng, Aijun, Zhu, Xiaoyu, Magnuson, Steven

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Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors von Chernov-Rogan, Tania, Li, Tianbo, Lu, Gang, Verschoof, Henry, Khakh, Kuldip, Jones, Steven W., Beresini, Maureen H., Liu, Chang, Ortwine, Daniel F., McKerrall, Steven J., Hackos, David H., Sutherlin, Daniel, Cohen, Charles J., Chen, Jun

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Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells von Koehler, Michael F. T, Bergeron, Philippe, Blackwood, Elizabeth M, Bowman, Krista, Clark, Kevin R, Firestein, Ron, Kiefer, James R, Maskos, Klaus, McCleland, Mark L, Orren, Linda, Salphati, Laurent, Schmidt, Steve, Schneider, Elisabeth V, Wu, Jiansheng, Beresini, Maureen H

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Lead identification of novel and selective TYK2 inhibitors von Liang, Jun, Tsui, Vickie, Van Abbema, Anne, Bao, Liang, Barrett, Kathy, Beresini, Maureen, Berezhkovskiy, Leo, Blair, Wade S., Chang, Christine, Driscoll, James, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Halladay, Jason, Johnson, Adam, Kohli, Pawan Bir, Lai, Yingjie, Liimatta, Marya, Mantik, Priscilla, Menghrajani, Kapil, Murray, Jeremy, Sambrone, Amy, Xiao, Yisong, Shia, Steven, Shin, Young, Smith, Jan, Sohn, Sue, Stanley, Mark, Ultsch, Mark, Zhang, Birong, Wu, Lawren C., Magnuson, Steven

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Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300 von Lai, Kwong Wah, Romero, F. Anthony, Tsui, Vickie, Beresini, Maureen H., de Leon Boenig, Gladys, Bronner, Sarah M., Chen, Kevin, Chen, Zhongguo, Choo, Edna F., Crawford, Terry D., Cyr, Patrick, Kaufman, Susan, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Ly, Justin, Murray, Jeremy, Shen, Weichao, Wai, John, Wang, Fei, Zhu, Caicai, Zhu, Xiaoyu, Magnuson, Steven

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