Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials von Albrecht, Brian K, Gehling, Victor S, Hewitt, Michael C, Vaswani, Rishi G, Côté, Alexandre, Leblanc, Yves, Nasveschuk, Christopher G, Bellon, Steve, Bergeron, Louise, Campbell, Robert, Cantone, Nico, Cooper, Michael R, Cummings, Richard T, Jayaram, Hariharan, Joshi, Shivangi, Mertz, Jennifer A, Neiss, Adrianne, Normant, Emmanuel, O’Meara, Michael, Pardo, Eneida, Poy, Florence, Sandy, Peter, Supko, Jeffrey, Sims, Robert J, Harmange, Jean-Christophe, Taylor, Alexander M, Audia, James E

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Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma von Conery, Andrew R, Centore, Richard C, Neiss, Adrianne, Keller, Patricia J, Joshi, Shivangi, Spillane, Kerry L, Sandy, Peter, Hatton, Charlie, Pardo, Eneida, Zawadzke, Laura, Bommi-Reddy, Archana, Gascoigne, Karen E, Bryant, Barbara M, Mertz, Jennifer A, Sims, Robert J

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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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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance von Crawford, Terry D., Vartanian, Steffan, Côté, Alexandre, Bellon, Steve, Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael, Huang, Hon-Ren, Kiefer, James R., Murray, Jeremy, Nasveschuk, Christopher G., Pardo, Eneida, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Taylor, Alexander M., Tsui, Vickie, Wang, Jian, Wang, Shumei, Zawadzke, Laura, Albrecht, Brian K., Magnuson, Steven R., Cochran, Andrea G., Stokoe, David

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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, Design, and Optimization of Isoxazole Azepine BET Inhibitors von Gehling, Victor S, Hewitt, Michael C, Vaswani, Rishi G, Leblanc, Yves, Côté, Alexandre, Nasveschuk, Christopher G, Taylor, Alexander M, Harmange, Jean-Christophe, Audia, James E, Pardo, Eneida, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A, Sims, Robert J, Bergeron, Louise, Bryant, Barbara M, Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Sankaranarayanan, Ravichandran, Yellapantula, Sreegouri, Bangalore Srinivasamurthy, Nandana, Birudukota, Swarnakumari, Albrecht, Brian K

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Correction: Bromodomain inhibition of the transcriptional coactivators CBP/EP300 as a therapeutic strategy to target the IRF4 network in multiple myeloma von Conery, Andrew R, Centore, Richard C, Neiss, Adrianne, Keller, Patricia J, Joshi, Shivangi, Spillane, Kerry L, Sandy, Peter, Hatton, Charlie, Pardo, Eneida, Zawadzke, Laura, Bommi-Reddy, Archana, Gascoigne, Karen E, Bryant, Barbara M, Mertz, Jennifer A, Sims, Robert J

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Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains von Taylor, Alexander M, Vaswani, Rishi G, Gehling, Victor S, Hewitt, Michael C, Leblanc, Yves, Audia, James E, Bellon, Steve, Cummings, Richard T, Côté, Alexandre, Harmange, Jean-Christophe, Jayaram, Hari, Joshi, Shivangi, Lora, Jose M, Mertz, Jennifer A, Neiss, Adrianne, Pardo, Eneida, Nasveschuk, Christopher G, Poy, Florence, Sandy, Peter, Setser, Jeremy W, Sims, Robert J, Tang, Yong, Albrecht, Brian K

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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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Abstract 3079: FT-6876, a potent and selective inhibitor of CBP/p300 with antitumor activity in AR-positive breast cancer von Caligiuri, Maureen, Williams, Grace L., Castro, Jennifer, Battalagine, Linda, Muskiewicz, Kristina, Wilker, Erik, Yao, Lili, Schiller, Shawn, Toms, Angela, Li, Ping, Pardo, Eneida, Graves, Bradford, Wood, Kenneth W., Guichard, Sylvie M.

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Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition von Ghosh, Srimoyee, Taylor, Alexander, Chin, Melissa, Huang, Hon-Ren, Conery, Andrew R., Mertz, Jennifer A., Salmeron, Andres, Dakle, Pranal J., Mele, Deanna, Cote, Alexandre, Jayaram, Hari, Setser, Jeremy W., Poy, Florence, Hatzivassiliou, Georgia, DeAlmeida-Nagata, Denise, Sandy, Peter, Hatton, Charlie, Romero, F. Anthony, Chiang, Eugene, Reimer, Thornik, Crawford, Terry, Pardo, Eneida, Watson, Venita G., Tsui, Vickie, Cochran, Andrea G., Zawadzke, Laura, Harmange, Jean-Christophe, Audia, James E., Bryant, Barbara M., Cummings, Richard T., Magnuson, Steven R., Grogan, Jane L., Bellon, Steve F., Albrecht, Brian K., Sims, Robert J., Lora, Jose M.

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FT-6876, a Potent and Selective Inhibitor of CBP/p300, is Active in Preclinical Models of Androgen Receptor-Positive Breast Cancer von Caligiuri, Maureen, Williams, Grace L., Castro, Jennifer, Battalagine, Linda, Wilker, Erik, Yao, Lili, Schiller, Shawn, Toms, Angela, Li, Ping, Pardo, Eneida, Graves, Bradford, Azofeifa, Joey, Chicas, Agustin, Herbertz, Torsten, Lai, Maria, Basken, Joel, Wood, Kenneth W., Xu, Qunli, Guichard, Sylvie M.

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Multiple versions of the A mating type locus of Coprinus cinereus are generated by three paralogous pairs of multiallelic homeobox genes von Pardo, E.H. (University of Oxford, Oxford, UK.), O'Shea, S.F, Casselton, L.A

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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 Subuni... von 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

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Development of methyl isoxazoleazepines as inhibitors of BET von Hewitt, Michael C, Leblanc, Yves, Gehling, Victor S, Vaswani, Rishi G, Côté, Alexandre, Nasveschuk, Christopher G, Taylor, Alexander M, Harmange, Jean-Christophe, Audia, James E, Pardo, Eneida, Cummings, Rich, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A, Sims, 3rd, Robert J, Bergeron, Louise, Bryant, Barbara M, Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Jayaran, Hariharan, Tang, Yong, Albrecht, Brian K

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The Impact of Variable Selection Coverage on Detection of Ligands from a DNA-Encoded Library Screen von McCarthy, Kelly A., Franklin, G. Joseph, Lancia, Jr, David R., Olbrot, Martin, Pardo, Eneida, O’Connell, Jonathan C., Kollmann, Christopher S.

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GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2) von Crawford, Terry D, Audia, James E, Bellon, Steve, Burdick, Daniel J, Bommi-Reddy, Archana, Côté, Alexandre, Cummings, Richard T, Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael, Huang, Hon-Ren, Jayaram, Hariharan, Jiang, Ying, Joshi, Shivangi, Kiefer, James R, Murray, Jeremy, Nasveschuk, Christopher G, Neiss, Arianne, Pardo, Eneida, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Taylor, Alexander M, Tsui, Vickie, Wang, Jian, Wang, Shumei, Wang, Yongyun, Xu, Zhaowu, Zawadzke, Laura, Zhu, Xiaoqin, Albrecht, Brian K, Magnuson, Steven R, Cochran, Andrea G

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Corrigendum to “Development of methyl isoxazoleazepines as inhibitors of BET” [Bioorg. Med. Chem. Lett. 25/9 (2015) 1842–1848] von Hewitt, Michael C., Leblanc, Yves, Gehling, Victor S., Vaswani, Rishi G., Côté, Alexandre, Nasveschuk, Christopher G., Taylor, Alexander M., Harmange, Jean-Christophe, Audia, James E., Pardo, Eneida, Cummings, Rich, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A., Sims, Robert J., Bergeron, Louise, Bryant, Barbara M., Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Tang, Yong, Albrecht, Brian K.

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Abstract A20: A leukemic model of acquired resistance to BET inhibition reveals a role for CBP/EP300 bromodomains in the regulation of c-MYC expression von Conery, Andrew R., Centore, Richard C., Hatton, Charlie, Neiss, Adrianne, Huang, Hon-Ren, Keller, Patricia J., Taylor, Alexander M., Cote, Alexandre, Hewitt, Michael C., Nasveschuk, Christopher G., Leblanc, Yves, Yao, Shihua, Pardo, Eneida, Zawadzke, Laura, Poy, Florence, Jayaram, Hari, Joshi, Shivangi, Sandy, Peter, Romero, Anthony, Crawford, Terry, Pastor, Richard, Lai, Tommy, Chen, Kevin, Wang, Jian, Magnuson, Steven, Albrecht, Brian K., Bellon, Steve, Bryant, Barbara M., Sims, Robert J.

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Abstract LB-237: In vitro and in vivo characterization of CPI-267203, a potent Inhibitor of bromodomain-containing proteins von Normant, Emmanuel, Cummings, Richard, Bellon, Steven, Bailey, Christopher, Albrecht, Brian, Hewitt, Michael, Pardo, Eneida, Campbell, Robert, Jayaram, Hari, Poy, Florence, Sandy, Peter, Gangurde, Pranoti

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