Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer
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
Published in Cancer research (Chicago, Ill.) (15.10.2017)
Published in Cancer research (Chicago, Ill.) (15.10.2017)
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Structural basis for dual-mode inhibition of the ABC transporter MsbA
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.
Published in Nature (London) (01.05.2018)
Published in Nature (London) (01.05.2018)
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Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists
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
Published in Nature structural & molecular biology (01.10.2017)
Published in Nature structural & molecular biology (01.10.2017)
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300
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
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands
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
Published in Nature communications (14.12.2020)
Published in Nature communications (14.12.2020)
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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)
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
Published in ACS medicinal chemistry letters (12.05.2016)
Published in ACS medicinal chemistry letters (12.05.2016)
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A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors
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
Published in Journal of medicinal chemistry (28.12.2017)
Published in Journal of medicinal chemistry (28.12.2017)
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USP7 small-molecule inhibitors interfere with ubiquitin binding
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.
Published in Nature (London) (26.10.2017)
Published in Nature (London) (26.10.2017)
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Disruption of IRE1α through its kinase domain attenuates multiple myeloma
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
Published in Proceedings of the National Academy of Sciences - PNAS (13.08.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (13.08.2019)
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Journal Article
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)
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
Published in Journal of medicinal chemistry (22.11.2017)
Published in Journal of medicinal chemistry (22.11.2017)
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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
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
Published in Journal of medicinal chemistry (13.06.2024)
Published in Journal of medicinal chemistry (13.06.2024)
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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains
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
Published in Journal of medicinal chemistry (09.06.2016)
Published in Journal of medicinal chemistry (09.06.2016)
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Journal Article
Design of Organo-Peptides As Bipartite PCSK9 Antagonists
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
Published in ACS chemical biology (21.02.2020)
Published in ACS chemical biology (21.02.2020)
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Journal Article
High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRAS G12C by Intact Protein MS and Targeted MRM
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
Published in Analytical chemistry (Washington) (18.01.2022)
Published in Analytical chemistry (Washington) (18.01.2022)
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Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors
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
Published in Proceedings of the National Academy of Sciences - PNAS (23.01.2018)
Published in Proceedings of the National Academy of Sciences - PNAS (23.01.2018)
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Journal Article
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells
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
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Journal Article
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300
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
Published in Bioorganic & medicinal chemistry letters (01.01.2018)
Published in Bioorganic & medicinal chemistry letters (01.01.2018)
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High throughput screening identifies novel, cell cycle‐arresting small molecule enhancers of transient protein expression
Meyer, Hermann‐Josef, Turincio, Rebecca, Ng, Shirley, Li, Juan, Wilson, Blair, Chan, Pamela, Zak, Mark, Reilly, Dorothea, Beresini, Maureen H., Wong, Athena W.
Published in Biotechnology progress (01.11.2017)
Published in Biotechnology progress (01.11.2017)
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GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1‑like
Wang, Shumei, Tsui, Vickie, Crawford, Terry D, Audia, James E, Burdick, Daniel J, Beresini, Maureen H, Côté, Alexandre, Cummings, Richard, Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael C, Huang, Hon-Ren, Jayaram, Hariharan, Jiang, Ying, Joshi, Shivangi, Murray, Jeremy, Nasveschuk, Christopher G, Pardo, Eneida, Poy, Florence, Romero, F. Anthony, Tang, Yong, Taylor, Alexander M, Wang, Jian, Xu, Zhaowu, Zawadzke, Laura E, Zhu, Xiaoyu, Albrecht, Brian K, Magnuson, Steven R, Bellon, Steve, Cochran, Andrea G
Published in Journal of medicinal chemistry (25.10.2018)
Published in Journal of medicinal chemistry (25.10.2018)
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Compound Transfer by Acoustic Droplet Ejection Promotes Quality and Efficiency in Ultra-High-Throughput Screening Campaigns
Dawes, Timothy D., Turincio, Rebecca, Jones, Steven W., Rodriguez, Richard A., Gadiagellan, Dhireshan, Thana, Peter, Clark, Kevin R., Gustafson, Amy E., Orren, Linda, Liimatta, Marya, Gross, Daniel P., Maurer, Till, Beresini, Maureen H.
Published in Journal of Laboratory Automation (01.02.2016)
Published in Journal of Laboratory Automation (01.02.2016)
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