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1. Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease

Author

Terrett, Jack A., primary, Ly, Justin Q., additional, Katavolos, Paula, additional, Hasselgren, Catrin, additional, Laing, Steven, additional, Zhong, Fiona, additional, Villemure, Elisia, additional, Déry, Martin, additional, Larouche-Gauthier, Robin, additional, Chen, Huifen, additional, Shore, Daniel G., additional, Lee, Wyne P., additional, Suto, Eric, additional, Johnson, Kevin, additional, Brooks, Marjory, additional, Stablein, Alyssa, additional, Beaumier, Francis, additional, Constantineau-Forget, Léa, additional, Grand-Maître, Chantal, additional, Lépissier, Luce, additional, Ciblat, Stéphane, additional, Sturino, Claudio, additional, Chen, Yong, additional, Hu, Baihua, additional, Elstrott, Justin, additional, Gandham, Vineela, additional, Joseph, Victory, additional, Booler, Helen, additional, Cain, Gary, additional, Chou, Carolina, additional, Fullerton, Aaron, additional, Lepherd, Michelle, additional, Stainton, Shannon, additional, Torres, Elizabeth, additional, Urban, Konnie, additional, Yu, Lanlan, additional, Zhong, Yu, additional, Bao, Linda, additional, Chou, Kang-Jye, additional, Lin, Jessica, additional, Zhang, Wei, additional, La, Hank, additional, Liu, Liling, additional, Mulder, Teresa, additional, Chen, Jun, additional, Chernov-Rogan, Tania, additional, Johnson, Adam R., additional, Hackos, David H., additional, Leahey, Rebecca, additional, Shields, Shannon D., additional, Balestrini, Alessia, additional, Riol-Blanco, Lorena, additional, Safina, Brian S., additional, Volgraf, Matthew, additional, Magnuson, Steven, additional, and Kakiuchi-Kiyota, Satoko, additional

Published
2024
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4. Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition

Author

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., III, and Lora, Jose M.

Published
2016
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5. Table S1 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, primary, Chan, Emily, primary, de la Cruz, Cecile, primary, Segal, Ehud, primary, Merchant, Mark, primary, Kharbanda, Samir, primary, Raisner, Ryan, primary, Haverty, Peter M., primary, Modrusan, Zora, primary, Ly, Justin, primary, Choo, Edna, primary, Kaufman, Susan, primary, Beresini, Maureen H., primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, and Gascoigne, Karen E., primary

Published
2023
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6. Figure S6 from CBP/p300 Drives the Differentiation of Regulatory T Cells through Transcriptional and Non-Transcriptional Mechanisms

Author

Castillo, Joseph, primary, Wu, Esther, primary, Lowe, Christopher, primary, Srinivasan, Shrividhya, primary, McCord, Ron, primary, Wagle, Marie-Claire, primary, Jayakar, Sangeeta, primary, Edick, Melissa Gonzalez, primary, Eastham-Anderson, Jeffrey, primary, Liu, Bonnie, primary, Hutchinson, Katherine E., primary, Jones, Wendell, primary, Stokes, Matthew P., primary, Tarighat, Somayeh S., primary, Holcomb, Thomas, primary, Glibicky, Andrew, primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, Huang, Shih-Min A., primary, Plaks, Vicki, primary, Giltnane, Jennifer M., primary, Lackner, Mark R., primary, and Mounir, Zineb, primary

Published
2023
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7. Figure S4 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, primary, Chan, Emily, primary, de la Cruz, Cecile, primary, Segal, Ehud, primary, Merchant, Mark, primary, Kharbanda, Samir, primary, Raisner, Ryan, primary, Haverty, Peter M., primary, Modrusan, Zora, primary, Ly, Justin, primary, Choo, Edna, primary, Kaufman, Susan, primary, Beresini, Maureen H., primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, and Gascoigne, Karen E., primary

Published
2023
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8. Note S1 from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, primary, Chan, Emily, primary, de la Cruz, Cecile, primary, Segal, Ehud, primary, Merchant, Mark, primary, Kharbanda, Samir, primary, Raisner, Ryan, primary, Haverty, Peter M., primary, Modrusan, Zora, primary, Ly, Justin, primary, Choo, Edna, primary, Kaufman, Susan, primary, Beresini, Maureen H., primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, and Gascoigne, Karen E., primary

Published
2023
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9. Supplementary Figure legends from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, primary, Chan, Emily, primary, de la Cruz, Cecile, primary, Segal, Ehud, primary, Merchant, Mark, primary, Kharbanda, Samir, primary, Raisner, Ryan, primary, Haverty, Peter M., primary, Modrusan, Zora, primary, Ly, Justin, primary, Choo, Edna, primary, Kaufman, Susan, primary, Beresini, Maureen H., primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, and Gascoigne, Karen E., primary

Published
2023
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10. Data from Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, primary, Chan, Emily, primary, de la Cruz, Cecile, primary, Segal, Ehud, primary, Merchant, Mark, primary, Kharbanda, Samir, primary, Raisner, Ryan, primary, Haverty, Peter M., primary, Modrusan, Zora, primary, Ly, Justin, primary, Choo, Edna, primary, Kaufman, Susan, primary, Beresini, Maureen H., primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, and Gascoigne, Karen E., primary

Published
2023
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11. Table S1 to S5 from CBP/p300 Drives the Differentiation of Regulatory T Cells through Transcriptional and Non-Transcriptional Mechanisms

Author

Castillo, Joseph, primary, Wu, Esther, primary, Lowe, Christopher, primary, Srinivasan, Shrividhya, primary, McCord, Ron, primary, Wagle, Marie-Claire, primary, Jayakar, Sangeeta, primary, Edick, Melissa Gonzalez, primary, Eastham-Anderson, Jeffrey, primary, Liu, Bonnie, primary, Hutchinson, Katherine E., primary, Jones, Wendell, primary, Stokes, Matthew P., primary, Tarighat, Somayeh S., primary, Holcomb, Thomas, primary, Glibicky, Andrew, primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, Huang, Shih-Min A., primary, Plaks, Vicki, primary, Giltnane, Jennifer M., primary, Lackner, Mark R., primary, and Mounir, Zineb, primary

Published
2023
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12. Data from CBP/p300 Drives the Differentiation of Regulatory T Cells through Transcriptional and Non-Transcriptional Mechanisms

Author

Castillo, Joseph, primary, Wu, Esther, primary, Lowe, Christopher, primary, Srinivasan, Shrividhya, primary, McCord, Ron, primary, Wagle, Marie-Claire, primary, Jayakar, Sangeeta, primary, Edick, Melissa Gonzalez, primary, Eastham-Anderson, Jeffrey, primary, Liu, Bonnie, primary, Hutchinson, Katherine E., primary, Jones, Wendell, primary, Stokes, Matthew P., primary, Tarighat, Somayeh S., primary, Holcomb, Thomas, primary, Glibicky, Andrew, primary, Romero, F. Anthony, primary, Magnuson, Steven, primary, Huang, Shih-Min A., primary, Plaks, Vicki, primary, Giltnane, Jennifer M., primary, Lackner, Mark R., primary, and Mounir, Zineb, primary

Published
2023
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13. Supplementary Table S1 from A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Author

Lau, Ted, primary, Chan, Emily, primary, Callow, Marinella, primary, Waaler, Jo, primary, Boggs, Jason, primary, Blake, Robert A., primary, Magnuson, Steven, primary, Sambrone, Amy, primary, Schutten, Melissa, primary, Firestein, Ron, primary, Machon, Ondrej, primary, Korinek, Vladimir, primary, Choo, Edna, primary, Diaz, Dolores, primary, Merchant, Mark, primary, Polakis, Paul, primary, Holsworth, Daniel D., primary, Krauss, Stefan, primary, and Costa, Mike, primary

Published
2023
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14. Data from A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Author

Lau, Ted, primary, Chan, Emily, primary, Callow, Marinella, primary, Waaler, Jo, primary, Boggs, Jason, primary, Blake, Robert A., primary, Magnuson, Steven, primary, Sambrone, Amy, primary, Schutten, Melissa, primary, Firestein, Ron, primary, Machon, Ondrej, primary, Korinek, Vladimir, primary, Choo, Edna, primary, Diaz, Dolores, primary, Merchant, Mark, primary, Polakis, Paul, primary, Holsworth, Daniel D., primary, Krauss, Stefan, primary, and Costa, Mike, primary

Published
2023
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15. Supplemental Data from Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

Author

McGrath, John P., primary, Williamson, Kaylyn E., primary, Balasubramanian, Srividya, primary, Odate, Shobu, primary, Arora, Shilpi, primary, Hatton, Charlie, primary, Edwards, Thomas M., primary, O'Brien, Thomas, primary, Magnuson, Steven, primary, Stokoe, David, primary, Daniels, Danette L., primary, Bryant, Barbara M., primary, and Trojer, Patrick, primary

Published
2023
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16. Supplementary Table 3 from A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Author

Lau, Ted, primary, Chan, Emily, primary, Callow, Marinella, primary, Waaler, Jo, primary, Boggs, Jason, primary, Blake, Robert A., primary, Magnuson, Steven, primary, Sambrone, Amy, primary, Schutten, Melissa, primary, Firestein, Ron, primary, Machon, Ondrej, primary, Korinek, Vladimir, primary, Choo, Edna, primary, Diaz, Dolores, primary, Merchant, Mark, primary, Polakis, Paul, primary, Holsworth, Daniel D., primary, Krauss, Stefan, primary, and Costa, Mike, primary

Published
2023
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17. Supplementary Figure S4 from A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Author

Lau, Ted, primary, Chan, Emily, primary, Callow, Marinella, primary, Waaler, Jo, primary, Boggs, Jason, primary, Blake, Robert A., primary, Magnuson, Steven, primary, Sambrone, Amy, primary, Schutten, Melissa, primary, Firestein, Ron, primary, Machon, Ondrej, primary, Korinek, Vladimir, primary, Choo, Edna, primary, Diaz, Dolores, primary, Merchant, Mark, primary, Polakis, Paul, primary, Holsworth, Daniel D., primary, Krauss, Stefan, primary, and Costa, Mike, primary

Published
2023
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18. Data from Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

Author

McGrath, John P., primary, Williamson, Kaylyn E., primary, Balasubramanian, Srividya, primary, Odate, Shobu, primary, Arora, Shilpi, primary, Hatton, Charlie, primary, Edwards, Thomas M., primary, O'Brien, Thomas, primary, Magnuson, Steven, primary, Stokoe, David, primary, Daniels, Danette L., primary, Bryant, Barbara M., primary, and Trojer, Patrick, primary

Published
2023
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19. Table S1 from Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

Author

McGrath, John P., primary, Williamson, Kaylyn E., primary, Balasubramanian, Srividya, primary, Odate, Shobu, primary, Arora, Shilpi, primary, Hatton, Charlie, primary, Edwards, Thomas M., primary, O'Brien, Thomas, primary, Magnuson, Steven, primary, Stokoe, David, primary, Daniels, Danette L., primary, Bryant, Barbara M., primary, and Trojer, Patrick, primary

Published
2023
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20. Supplementary Data from A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth

Author

Lau, Ted, primary, Chan, Emily, primary, Callow, Marinella, primary, Waaler, Jo, primary, Boggs, Jason, primary, Blake, Robert A., primary, Magnuson, Steven, primary, Sambrone, Amy, primary, Schutten, Melissa, primary, Firestein, Ron, primary, Machon, Ondrej, primary, Korinek, Vladimir, primary, Choo, Edna, primary, Diaz, Dolores, primary, Merchant, Mark, primary, Polakis, Paul, primary, Holsworth, Daniel D., primary, Krauss, Stefan, primary, and Costa, Mike, primary

Published
2023
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21. GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1

Author

Taylor, Alexander M., primary, Bailey, Chris, additional, Belmont, Lisa D., additional, Campbell, Robert, additional, Cantone, Nico, additional, Côté, Alexandre, additional, Crawford, Terry D., additional, Cummings, Richard, additional, DeMent, Kevin, additional, Duplessis, Martin, additional, Flynn, Megan, additional, Good, Andrew C., additional, Huang, Hon-Ren, additional, Joshi, Shivangi, additional, Leblanc, Yves, additional, Murray, Jeremy, additional, Nasveschuk, Christopher G., additional, Neiss, Adrianne, additional, Poy, Florence, additional, Romero, F. Anthony, additional, Sandy, Peter, additional, Tang, Yong, additional, Tsui, Vickie, additional, Zawadzke, Laura, additional, Sims, Robert J., additional, Audia, James E., additional, Bellon, Steven F., additional, Magnuson, Steven R., additional, Albrecht, Brian K., additional, and Cochran, Andrea G., additional

Published
2022
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22. Lead identification of novel and selective TYK2 inhibitors

Author

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., and Magnuson, Steven

Published
2013
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24. Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy

Author

Terrett, Jack A., primary, Chen, Huifen, additional, Shore, Daniel G., additional, Villemure, Elisia, additional, Larouche-Gauthier, Robin, additional, Déry, Martin, additional, Beaumier, Francis, additional, Constantineau-Forget, Léa, additional, Grand-Maître, Chantal, additional, Lépissier, Luce, additional, Ciblat, Stéphane, additional, Sturino, Claudio, additional, Chen, Yong, additional, Hu, Baihua, additional, Lu, Aijun, additional, Wang, Yunli, additional, Cridland, Andrew P., additional, Ward, Stuart I., additional, Hackos, David H., additional, Reese, Rebecca M., additional, Shields, Shannon D., additional, Chen, Jun, additional, Balestrini, Alessia, additional, Riol-Blanco, Lorena, additional, Lee, Wyne P., additional, Liu, John, additional, Suto, Eric, additional, Wu, Xiumin, additional, Zhang, Juan, additional, Ly, Justin Q., additional, La, Hank, additional, Johnson, Kevin, additional, Baumgardner, Matt, additional, Chou, Kang-Jye, additional, Rohou, Alexis, additional, Rougé, Lionel, additional, Safina, Brian S., additional, Magnuson, Steven, additional, and Volgraf, Matthew, additional

Published
2021
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25. A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment

Author

Balestrini, Alessia, primary, Joseph, Victory, additional, Dourado, Michelle, additional, Reese, Rebecca M., additional, Shields, Shannon D., additional, Rougé, Lionel, additional, Bravo, Daniel D., additional, Chernov-Rogan, Tania, additional, Austin, Cary D., additional, Chen, Huifen, additional, Wang, Lan, additional, Villemure, Elisia, additional, Shore, Daniel G.M., additional, Verma, Vishal A., additional, Hu, Baihua, additional, Chen, Yong, additional, Leong, Laurie, additional, Bjornson, Chris, additional, Hötzel, Kathy, additional, Gogineni, Alvin, additional, Lee, Wyne P., additional, Suto, Eric, additional, Wu, Xiumin, additional, Liu, John, additional, Zhang, Juan, additional, Gandham, Vineela, additional, Wang, Jianyong, additional, Payandeh, Jian, additional, Ciferri, Claudio, additional, Estevez, Alberto, additional, Arthur, Christopher P., additional, Kortmann, Jens, additional, Wong, Ryan L., additional, Heredia, Jose E., additional, Doerr, Jonas, additional, Jung, Min, additional, Vander Heiden, Jason A., additional, Roose-Girma, Merone, additional, Tam, Lucinda, additional, Barck, Kai H., additional, Carano, Richard A.D., additional, Ding, Han Ting, additional, Brillantes, Bobby, additional, Tam, Christine, additional, Yang, Xiaoying, additional, Gao, Simon S., additional, Ly, Justin Q., additional, Liu, Liling, additional, Chen, Liuxi, additional, Liederer, Bianca M., additional, Lin, Joseph H., additional, Magnuson, Steven, additional, Chen, Jun, additional, Hackos, David H., additional, Elstrott, Justin, additional, Rohou, Alexis, additional, Safina, Brian S., additional, Volgraf, Matthew, additional, Bauer, Rebecca N., additional, and Riol-Blanco, Lorena, additional

Published
2021
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27. CBPi_manuscript_Supplemental_Data_Table_1_(11-22-19) - Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs

Author

Katavolos, Paula, Cain, Gary, Farman, Cindy, F. Anthony Romero, Magnuson, Steven, Ly, Justin Q., Choo, Edna F., Katakam, Anand Kumar, Andaya, Roxanne, and Maher, Jonathan

Subjects
FOS: Clinical medicine, 111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified
Abstract

CBPi_manuscript_Supplemental_Data_Table_1_(11-22-19) for Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs by Paula Katavolos, Gary Cain, Cindy Farman, F. Anthony Romero, Steven Magnuson, Justin Q. Ly, Edna F. Choo, Anand Kumar Katakam, Roxanne Andaya and Jonathan Maher in Toxicologic Pathology

Published
2020
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28. Cyclopentannulation by an iterative process of sequential Claisen rearrangement and enyne radical closure: routes to triquinane and propellane systems and use in the synthesis of (plus or minus)-ceratopicanol

Author

Clive, D.L.J., Magnuson, Steven R., Manning, Hartford W., and Mayhew, Darrin L.

Subjects
Radicals (Chemistry) -- Research, Alcohols -- Research, Propellanes -- Research, Ring formation (Chemistry) -- Research, Acetylene -- Research, Rearrangements (Chemistry) -- Research, Biological sciences, Chemistry
Abstract

An iterative method, utilizing Claisen rearrangement and enyne radical closure, is employed in cyclopentannulation of cyclic allylic alcohol giving triquinane and propellane compounds. An improved method is also able to synthesize sesquiterpene (plus or minus)-ceratopicanol. The allylic alcohol first undergoes Claisen rearrangement and subsequent homologation into an enyne. Enyne is converted into vinyl stannane, and finally ketone, upon treatment with stannyl radicals. The synthetic allylic alcohols are stereochemically converted into their epimers, hence repeating the process.

Published
1996

30. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300

Author

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, and Magnuson, Steven

Published
2018
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31. CBP/p300 Drives the Differentiation of Regulatory T Cells through Transcriptional and Non-Transcriptional Mechanisms

Author

Castillo, Joseph, primary, Wu, Esther, additional, Lowe, Christopher, additional, Srinivasan, Shrividhya, additional, McCord, Ron, additional, Wagle, Marie-Claire, additional, Jayakar, Sangeeta, additional, Edick, Melissa Gonzalez, additional, Eastham-Anderson, Jeffrey, additional, Liu, Bonnie, additional, Hutchinson, Katherine E., additional, Jones, Wendell, additional, Stokes, Matthew P., additional, Tarighat, Somayeh S., additional, Holcomb, Thomas, additional, Glibicky, Andrew, additional, Romero, F. Anthony, additional, Magnuson, Steven, additional, Huang, Shih-Min A., additional, Plaks, Vicki, additional, Giltnane, Jennifer M., additional, Lackner, Mark R., additional, and Mounir, Zineb, additional

Published
2019
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32. Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model

Author

Liang, Jun, Van Abbema, Anne, Balazs, Mercedesz, Barrett, Kathy, Berezhkovsky, Leo, Blair, Wade S., Chang, Christine, Delarosa, Donnie, DeVoss, Jason, Driscoll, Jim, Eigenbrot, Charles, Goodacre, Simon, Ghilardi, Nico, MacLeod, Calum, Johnson, Adam, Bir Kohli, Pawan, Lai, Yingjie, Lin, Zhonghua, Mantik, Priscilla, Menghrajani, Kapil, Nguyen, Hieu, Peng, Ivan, Sambrone, Amy, Shia, Steven, Smith, Jan, Sohn, Sue, Tsui, Vickie, Ultsch, Mark, Williams, Karen, Wu, Lawren C., Yang, Wenqian, Zhang, Birong, and Magnuson, Steven

Published
2017
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33. Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance

Author

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., and Stokoe, David

Published
2017
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34. 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

Author

Wang, Shumei, primary, Tsui, Vickie, additional, Crawford, Terry D., additional, Audia, James E., additional, Burdick, Daniel J., additional, Beresini, Maureen H., additional, Côté, Alexandre, additional, Cummings, Richard, additional, Duplessis, Martin, additional, Flynn, E. Megan, additional, Hewitt, Michael C., additional, Huang, Hon-Ren, additional, Jayaram, Hariharan, additional, Jiang, Ying, additional, Joshi, Shivangi, additional, Murray, Jeremy, additional, Nasveschuk, Christopher G., additional, Pardo, Eneida, additional, Poy, Florence, additional, Romero, F. Anthony, additional, Tang, Yong, additional, Taylor, Alexander M., additional, Wang, Jian, additional, Xu, Zhaowu, additional, Zawadzke, Laura E., additional, Zhu, Xiaoyu, additional, Albrecht, Brian K., additional, Magnuson, Steven R., additional, Bellon, Steve, additional, and Cochran, Andrea G., additional

Published
2018
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36. A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors

Author

Bronner, Sarah M., primary, Murray, Jeremy, additional, Romero, F. Anthony, additional, Lai, Kwong Wah, additional, Tsui, Vickie, additional, Cyr, Patrick, additional, Beresini, Maureen H., additional, de leon Boenig, Gladys, additional, Chen, Zhongguo, additional, Choo, Edna F., additional, Clark, Kevin R., additional, Crawford, Terry D., additional, Jayaram, Hariharan, additional, Kaufman, Susan, additional, Li, Ruina, additional, Li, Yingjie, additional, Liao, Jiangpeng, additional, Liang, Xiaorong, additional, Liu, Wenfeng, additional, Ly, Justin, additional, Maher, Jonathan, additional, Wai, John, additional, Wang, Fei, additional, Zheng, Aijun, additional, Zhu, Xiaoyu, additional, and Magnuson, Steven, additional

Published
2017
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37. Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

Author

Jin, Lingyan, primary, Garcia, Jesse, additional, Chan, Emily, additional, de la Cruz, Cecile, additional, Segal, Ehud, additional, Merchant, Mark, additional, Kharbanda, Samir, additional, Raisner, Ryan, additional, Haverty, Peter M., additional, Modrusan, Zora, additional, Ly, Justin, additional, Choo, Edna, additional, Kaufman, Susan, additional, Beresini, Maureen H., additional, Romero, F. Anthony, additional, Magnuson, Steven, additional, and Gascoigne, Karen E., additional

Published
2017
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38. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)

Author

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

Published
2017
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39. GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2)

Author

Crawford, Terry D., primary, Audia, James E., additional, Bellon, Steve, additional, Burdick, Daniel J., additional, Bommi-Reddy, Archana, additional, Côté, Alexandre, additional, Cummings, Richard T., additional, Duplessis, Martin, additional, Flynn, E. Megan, additional, Hewitt, Michael, additional, Huang, Hon-Ren, additional, Jayaram, Hariharan, additional, Jiang, Ying, additional, Joshi, Shivangi, additional, Kiefer, James R., additional, Murray, Jeremy, additional, Nasveschuk, Christopher G., additional, Neiss, Arianne, additional, Pardo, Eneida, additional, Romero, F. Anthony, additional, Sandy, Peter, additional, Sims, Robert J., additional, Tang, Yong, additional, Taylor, Alexander M., additional, Tsui, Vickie, additional, Wang, Jian, additional, Wang, Shumei, additional, Wang, Yongyun, additional, Xu, Zhaowu, additional, Zawadzke, Laura, additional, Zhu, Xiaoqin, additional, Albrecht, Brian K., additional, Magnuson, Steven R., additional, and Cochran, Andrea G., additional

Published
2017
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43. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300

Author

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

Published
2016
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44. Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Author

Crawford, Terry D., primary, Tsui, Vickie, additional, Flynn, E. Megan, additional, Wang, Shumei, additional, Taylor, Alexander M., additional, Côté, Alexandre, additional, Audia, James E., additional, Beresini, Maureen H., additional, Burdick, Daniel J., additional, Cummings, Richard, additional, Dakin, Les A., additional, Duplessis, Martin, additional, Good, Andrew C., additional, Hewitt, Michael C., additional, Huang, Hon-Ren, additional, Jayaram, Hariharan, additional, Kiefer, James R., additional, Jiang, Ying, additional, Murray, Jeremy, additional, Nasveschuk, Christopher G., additional, Pardo, Eneida, additional, Poy, Florence, additional, Romero, F. Anthony, additional, Tang, Yong, additional, Wang, Jian, additional, Xu, Zhaowu, additional, Zawadzke, Laura E., additional, Zhu, Xiaoyu, additional, Albrecht, Brian K., additional, Magnuson, Steven R., additional, Bellon, Steve, additional, and Cochran, Andrea G., additional

Published
2016
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45. Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes

Author

McGrath, John P., primary, Williamson, Kaylyn E., additional, Balasubramanian, Srividya, additional, Odate, Shobu, additional, Arora, Shilpi, additional, Hatton, Charlie, additional, Edwards, Thomas M., additional, O'Brien, Thomas, additional, Magnuson, Steven, additional, Stokoe, David, additional, Daniels, Danette L., additional, Bryant, Barbara M., additional, and Trojer, Patrick, additional

Published
2016
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46. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

Author

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

Published
2016
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48. A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors

Author

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, and Magnuson, Steven

Abstract

The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region and then building into the LPF shelf. Herein, we report the “hybridization” of a variety of KAc-binding fragments with a tetrahydroquinoline scaffold that makes optimal interactions with the LPF shelf, imparting enhanced potency and selectivity to the hybridized ligand. To demonstrate the utility of our hybridization approach, two analogues containing unique Asn binders and the optimized tetrahydroquinoline moiety were rapidly optimized to yield single-digit nanomolar inhibitors of CBP with exquisite selectivity over BRD4(1) and the broader bromodomain family.

Published
2024
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50. 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

Author

Conery, Andrew R., primary, Centore, Richard C., additional, Hatton, Charlie, additional, Neiss, Adrianne, additional, Huang, Hon-Ren, additional, Keller, Patricia J., additional, Taylor, Alexander M., additional, Cote, Alexandre, additional, Hewitt, Michael C., additional, Nasveschuk, Christopher G., additional, Leblanc, Yves, additional, Yao, Shihua, additional, Pardo, Eneida, additional, Zawadzke, Laura, additional, Poy, Florence, additional, Jayaram, Hari, additional, Joshi, Shivangi, additional, Sandy, Peter, additional, Romero, Anthony, additional, Crawford, Terry, additional, Pastor, Richard, additional, Lai, Tommy, additional, Chen, Kevin, additional, Wang, Jian, additional, Magnuson, Steven, additional, Albrecht, Brian K., additional, Bellon, Steve, additional, Bryant, Barbara M., additional, and Sims, Robert J., additional

Published
2015
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