Enhancer Activity Requires CBP/P300 Bromodomain-Dependent Histone H3K27 Acetylation
Raisner, Ryan, Kharbanda, Samir, Jin, Lingyan, Jeng, Edwin, Chan, Emily, Merchant, Mark, Haverty, Peter M., Bainer, Russell, Cheung, Tommy, Arnott, David, Flynn, E. Megan, Romero, F. Anthony, Magnuson, Steven, Gascoigne, Karen E.
Published in Cell reports (Cambridge) (14.08.2018)
Published in Cell reports (Cambridge) (14.08.2018)
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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
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Published in Cancer research (Chicago, Ill.) (15.10.2017)
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A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation―Driven Colorectal Tumor Growth
LAU, Ted, CHAN, Emily, MACHON, Ondrej, KORINEK, Vladimir, CHOO, Edna, DIAZ, Dolores, MERCHANT, Mark, POLAKIS, Paul, HOLSWORTH, Daniel D, KRAUSS, Stefan, COSTA, Mike, CALLOW, Marinella, WAALER, Jo, BOGGS, Jason, BLAKE, Robert A, MAGNUSON, Steven, SAMBRONE, Amy, SCHUTTEN, Melissa, FIRESTEIN, Ron
Published in Cancer research (Chicago, Ill.) (15.05.2013)
Published in Cancer research (Chicago, Ill.) (15.05.2013)
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Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes
McGrath, John P, Williamson, Kaylyn E, Balasubramanian, Srividya, Odate, Shobu, Arora, Shilpi, Hatton, Charlie, Edwards, Thomas M, O'Brien, Thomas, Magnuson, Steven, Stokoe, David, Daniels, Danette L, Bryant, Barbara M, Trojer, Patrick
Published in Cancer research (Chicago, Ill.) (01.04.2016)
Published in Cancer research (Chicago, Ill.) (01.04.2016)
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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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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1
Taylor, Alexander M., Bailey, Chris, Belmont, Lisa D., Campbell, Robert, Cantone, Nico, Côté, Alexandre, Crawford, Terry D., Cummings, Richard, DeMent, Kevin, Duplessis, Martin, Flynn, Megan, Good, Andrew C., Huang, Hon-Ren, Joshi, Shivangi, Leblanc, Yves, Murray, Jeremy, Nasveschuk, Christopher G., Neiss, Adrianne, Poy, Florence, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Tsui, Vickie, Zawadzke, Laura, Sims, Robert J., Audia, James E., Bellon, Steven F., Magnuson, Steven R., Albrecht, Brian K., Cochran, Andrea G.
Published in Journal of medicinal chemistry (25.08.2022)
Published in Journal of medicinal chemistry (25.08.2022)
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Discovery of Potent and Selective Pyrazolopyrimidine Janus Kinase 2 Inhibitors
Hanan, Emily J, van Abbema, Anne, Barrett, Kathy, Blair, Wade S, Blaney, Jeff, Chang, Christine, Eigenbrot, Charles, Flynn, Sean, Gibbons, Paul, Hurley, Christopher A, Kenny, Jane R, Kulagowski, Janusz, Lee, Leslie, Magnuson, Steven R, Morris, Claire, Murray, Jeremy, Pastor, Richard M, Rawson, Tom, Siu, Michael, Ultsch, Mark, Zhou, Aihe, Sampath, Deepak, Lyssikatos, Joseph P
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation
de Almeida Nagata, Denise E., Chiang, Eugene Y., Jhunjhunwala, Suchit, Caplazi, Patrick, Arumugam, Vidhyalakshmi, Modrusan, Zora, Chan, Emily, Merchant, Mark, Jin, Lingyan, Arnott, David, Romero, F. Anthony, Magnuson, Steven, Gascoigne, Karen E., Grogan, Jane L.
Published in Cell reports (Cambridge) (02.04.2019)
Published in Cell reports (Cambridge) (02.04.2019)
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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance
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
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition
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.
Published in The Journal of biological chemistry (17.06.2016)
Published in The Journal of biological chemistry (17.06.2016)
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A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors
Sohn, Sue J, Barrett, Kathy, Van Abbema, Anne, Chang, Christine, Kohli, Pawan Bir, Kanda, Hidenobu, Smith, Janice, Lai, Yingjie, Zhou, Aihe, Zhang, Birong, Yang, Wenqian, Williams, Karen, Macleod, Calum, Hurley, Christopher A, Kulagowski, Janusz J, Lewin-Koh, Nicholas, Dengler, Hart S, Johnson, Adam R, Ghilardi, Nico, Zak, Mark, Liang, Jun, Blair, Wade S, Magnuson, Steven, Wu, Lawren C
Published in The Journal of immunology (1950) (01.09.2013)
Published in The Journal of immunology (1950) (01.09.2013)
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Lead identification of novel and selective TYK2 inhibitors
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
Published in European journal of medicinal chemistry (01.09.2013)
Published in European journal of medicinal chemistry (01.09.2013)
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Discovery of Selective 4‑Amino-pyridopyrimidine Inhibitors of MAP4K4 Using Fragment-Based Lead Identification and Optimization
Crawford, Terry D, Ndubaku, Chudi O, Chen, Huifen, Boggs, Jason W, Bravo, Brandon J, DeLaTorre, Kelly, Giannetti, Anthony M, Gould, Stephen E, Harris, Seth F, Magnuson, Steven R, McNamara, Erin, Murray, Lesley J, Nonomiya, Jim, Sambrone, Amy, Schmidt, Stephen, Smyczek, Tanya, Stanley, Mark, Vitorino, Philip, Wang, Lan, West, Kristina, Wu, Ping, Ye, Weilan
Published in Journal of medicinal chemistry (24.04.2014)
Published in Journal of medicinal chemistry (24.04.2014)
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Lead Optimization of a 4‑Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors
Liang, Jun, van Abbema, Anne, Balazs, Mercedesz, Barrett, Kathy, Berezhkovsky, Leo, Blair, Wade, Chang, Christine, Delarosa, Donnie, DeVoss, Jason, Driscoll, Jim, Eigenbrot, Charles, Ghilardi, Nico, Gibbons, Paul, Halladay, Jason, Johnson, Adam, Kohli, Pawan Bir, Lai, Yingjie, Liu, Yanzhou, Lyssikatos, Joseph, Mantik, Priscilla, Menghrajani, Kapil, Murray, Jeremy, Peng, Ivan, Sambrone, Amy, Shia, Steven, Shin, Young, Smith, Jan, Sohn, Sue, Tsui, Vickie, Ultsch, Mark, Wu, Lawren C, Xiao, Yisong, Yang, Wenqian, Young, Judy, Zhang, Birong, Zhu, Bing-yan, Magnuson, Steven
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
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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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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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Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors
Burdick, Daniel J., Wang, Shumei, Heise, Christopher, Pan, Borlan, Drummond, Jake, Yin, JianPing, Goeser, Lauren, Magnuson, Steven, Blaney, Jeff, Moffat, John, Wang, Weiru, Chen, Huifen
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
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Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors
Wang, Lan, Stanley, Mark, Boggs, Jason W., Crawford, Terry D., Bravo, Brandon J., Giannetti, Anthony M., Harris, Seth F., Magnuson, Steven R., Nonomiya, Jim, Schmidt, Stephen, Wu, Ping, Ye, Weilan, Gould, Stephen E., Murray, Lesley J., Ndubaku, Chudi O., Chen, Huifen
Published in Bioorganic & medicinal chemistry letters (15.09.2014)
Published in Bioorganic & medicinal chemistry letters (15.09.2014)
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GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2)
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
Published in ACS medicinal chemistry letters (13.07.2017)
Published in ACS medicinal chemistry letters (13.07.2017)
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