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166 results on '"Faivre, Emily"'

1. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Author

Faivre, Emily J., McDaniel, Keith F., Albert, Daniel H., Mantena, Srinivasa R., Plotnik, Joshua P., Wilcox, Denise, Zhang, Lu, Bui, Mai H., Sheppard, Geoge, Wang, Le, Sehgal, Vasudha, Lin, Xiaoyu, Huang, Xiaoli, Lu, Xin, Uziel, Tamar, Hessler, Paul, and Lam, Lloyd T.

Subjects
Prostate cancer -- Care and treatment -- Genetic aspects, Chemical inhibitors -- Usage -- Health aspects, Proteins -- Physiological aspects, Epigenetic inheritance -- Health aspects, Environmental issues, Science and technology, Zoology and wildlife conservation
Abstract

Proteins of the bromodomain and extra-terminal (BET) domain family are epigenetic readers that bind acetylated histones through their bromodomains to regulate gene transcription. Dual-bromodomain BET inhibitors (DbBi) that bind with similar affinities to the first (BD1) and second (BD2) bromodomains of BRD2, BRD3, BRD4 and BRDt have displayed modest clinical activity in monotherapy cancer trials. A reduced number of thrombocytes in the blood (thrombocytopenia) as well as symptoms of gastrointestinal toxicity are dose-limiting adverse events for some types of DbBi.sup.1-5. Given that similar haematological and gastrointestinal defects were observed after genetic silencing of Brd4 in mice.sup.6, the platelet and gastrointestinal toxicities may represent on-target activities associated with BET inhibition. The two individual bromodomains in BET family proteins may have distinct functions.sup.7-9 and different cellular phenotypes after pharmacological inhibition of one or both bromodomains have been reported.sup.10,11, suggesting that selectively targeting one of the bromodomains may result in a different efficacy and tolerability profile compared with DbBi. Available compounds that are selective to individual domains lack sufficient potency and the pharmacokinetics properties that are required for in vivo efficacy and tolerability assessment.sup.10-13. Here we carried out a medicinal chemistry campaign that led to the discovery of ABBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-075.sup.14. Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy. ABBV-744, a selective inhibitor of the BD2 domains of BET family proteins, is effective against prostate cancer in mouse xenograft models, with lower toxicities than the dual-bromodomain BET inhibitor ABBV-075., Author(s): Emily J. Faivre [sup.1] , Keith F. McDaniel [sup.1] , Daniel H. Albert [sup.1] , Srinivasa R. Mantena [sup.2] , Joshua P. Plotnik [sup.1] , Denise Wilcox [sup.1] , [...]

Published
2020
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2. A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver.

Author

Suzawa, Miyuki, Miranda, Diego A, Ramos, Karmela A, Ang, Kenny K-H, Faivre, Emily J, Wilson, Christopher G, Caboni, Laura, Arkin, Michelle R, Kim, Yeong-Sang, Fletterick, Robert J, Diaz, Aaron, Schneekloth, John S, and Ingraham, Holly A

Subjects
Cells, Cultured, Hepatocytes, Animals, Humans, Mice, Mice, SCID, Tannins, Receptors, Cytoplasmic and Nuclear, Enzyme Inhibitors, Drug Evaluation, Preclinical, Gene Expression Profiling, Inhibitory Concentration 50, Sumoylation, NASH, NR5As, cell biology, human, human biology, medicine, mouse, phenotypic screen, primary hepatocytes, sumoylation, tannic acid, Cells, Cultured, SCID, Receptors, Cytoplasmic and Nuclear, Drug Evaluation, Preclinical, Biotechnology, Genetics, Digestive Diseases, Liver Disease, 5.1 Pharmaceuticals, Biochemistry and Cell Biology
Abstract

SUMO-modification of nuclear proteins has profound effects on gene expression. However, non-toxic chemical tools that modulate sumoylation in cells are lacking. Here, to identify small molecule sumoylation inhibitors we developed a cell-based screen that focused on the well-sumoylated substrate, human Liver Receptor Homolog-1 (hLRH-1, NR5A2). Our primary gene-expression screen assayed two SUMO-sensitive transcripts, APOC3 and MUC1, that are upregulated by SUMO-less hLRH-1 or by siUBC9 knockdown, respectively. A polyphenol, tannic acid (TA) emerged as a potent sumoylation inhibitor in vitro (IC50 = 12.8 µM) and in cells. TA also increased hLRH-1 occupancy on SUMO-sensitive transcripts. Most significantly, when tested in humanized mouse primary hepatocytes, TA inhibits hLRH-1 sumoylation and induces SUMO-sensitive genes, thereby recapitulating the effects of expressing SUMO-less hLRH-1 in mouse liver. Our findings underscore the benefits of phenotypic screening for targeting post-translational modifications, and illustrate the potential utility of TA for probing the cellular consequences of sumoylation.

Published
2015

3. Data from Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Author

Lam, Lloyd T., primary, Lin, Xiaoyu, primary, Faivre, Emily J., primary, Yang, Ziping, primary, Huang, Xiaoli, primary, Wilcox, Denise M., primary, Bellin, Richard J., primary, Jin, Sha, primary, Tahir, Stephen K., primary, Mitten, Michael, primary, Magoc, Terry, primary, Bhathena, Anahita, primary, Kati, Warren M., primary, Albert, Daniel H., primary, Shen, Yu, primary, and Uziel, Tamar, primary

Published
2023
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5. Supplementary Figures 1-3 from Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Author

Lam, Lloyd T., primary, Lin, Xiaoyu, primary, Faivre, Emily J., primary, Yang, Ziping, primary, Huang, Xiaoli, primary, Wilcox, Denise M., primary, Bellin, Richard J., primary, Jin, Sha, primary, Tahir, Stephen K., primary, Mitten, Michael, primary, Magoc, Terry, primary, Bhathena, Anahita, primary, Kati, Warren M., primary, Albert, Daniel H., primary, Shen, Yu, primary, and Uziel, Tamar, primary

Published
2023
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7. Figure S2 from Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Author

Zhang, Lu, primary, Cai, Tianyu, primary, Lin, Xiaoyu, primary, Huang, Xiaoli, primary, Bui, Mai H., primary, Plotnik, Joshua P., primary, Bellin, Richard J., primary, Faivre, Emily J., primary, Kuruvilla, Vinitha M., primary, Lam, Lloyd T., primary, Lu, Xin, primary, Zha, Zheng, primary, Feng, Weiguo, primary, Hessler, Paul, primary, Uziel, Tamar, primary, Zhang, Qi, primary, Cavazos, Antonio, primary, Han, Lina, primary, Ferguson, Debra C., primary, Mehta, Gaurav, primary, Shanmugavelandy, Sriram S., primary, Magoc, Terrance J., primary, Rowe, Jenny, primary, Goodwin, Neal C., primary, Dorritie, Kathleen A., primary, Boyiadzis, Michael, primary, Albert, Daniel H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, Konopleva, Marina, primary, and Shen, Yu, primary

Published
2023
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12. Supplementary Figure Legends from Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Author

Lam, Lloyd T., primary, Lin, Xiaoyu, primary, Faivre, Emily J., primary, Yang, Ziping, primary, Huang, Xiaoli, primary, Wilcox, Denise M., primary, Bellin, Richard J., primary, Jin, Sha, primary, Tahir, Stephen K., primary, Mitten, Michael, primary, Magoc, Terry, primary, Bhathena, Anahita, primary, Kati, Warren M., primary, Albert, Daniel H., primary, Shen, Yu, primary, and Uziel, Tamar, primary

Published
2023
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14. Table S1 from Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Author

Zhang, Lu, primary, Cai, Tianyu, primary, Lin, Xiaoyu, primary, Huang, Xiaoli, primary, Bui, Mai H., primary, Plotnik, Joshua P., primary, Bellin, Richard J., primary, Faivre, Emily J., primary, Kuruvilla, Vinitha M., primary, Lam, Lloyd T., primary, Lu, Xin, primary, Zha, Zheng, primary, Feng, Weiguo, primary, Hessler, Paul, primary, Uziel, Tamar, primary, Zhang, Qi, primary, Cavazos, Antonio, primary, Han, Lina, primary, Ferguson, Debra C., primary, Mehta, Gaurav, primary, Shanmugavelandy, Sriram S., primary, Magoc, Terrance J., primary, Rowe, Jenny, primary, Goodwin, Neal C., primary, Dorritie, Kathleen A., primary, Boyiadzis, Michael, primary, Albert, Daniel H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, Konopleva, Marina, primary, and Shen, Yu, primary

Published
2023
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15. Supplementary Data from Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Author

Zhang, Lu, primary, Cai, Tianyu, primary, Lin, Xiaoyu, primary, Huang, Xiaoli, primary, Bui, Mai H., primary, Plotnik, Joshua P., primary, Bellin, Richard J., primary, Faivre, Emily J., primary, Kuruvilla, Vinitha M., primary, Lam, Lloyd T., primary, Lu, Xin, primary, Zha, Zheng, primary, Feng, Weiguo, primary, Hessler, Paul, primary, Uziel, Tamar, primary, Zhang, Qi, primary, Cavazos, Antonio, primary, Han, Lina, primary, Ferguson, Debra C., primary, Mehta, Gaurav, primary, Shanmugavelandy, Sriram S., primary, Magoc, Terrance J., primary, Rowe, Jenny, primary, Goodwin, Neal C., primary, Dorritie, Kathleen A., primary, Boyiadzis, Michael, primary, Albert, Daniel H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, Konopleva, Marina, primary, and Shen, Yu, primary

Published
2023
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16. Supplemental figure 7 & 8 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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17. Supplemental figure 12 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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18. 'Supplemental figure 2 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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19. Supplemental figure 14 to 17 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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20. Data from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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21. Supplemental table 2 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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22. Supplemental figure 9 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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23. Supplemental figure 10 & 11 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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24. Supplemental table 4 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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25. Supplemental figure 4 & 5 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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26. Supplemental table 3 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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27. Supplemental figure 6 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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28. Supplemental table 1 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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29. Supplemental figure legends from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

Bui, Mai H., primary, Lin, Xiaoyu, primary, Albert, Daniel H., primary, Li, Leiming, primary, Lam, Lloyd T., primary, Faivre, Emily J., primary, Warder, Scott E., primary, Huang, Xiaoli, primary, Wilcox, Denise, primary, Donawho, Cherrie K., primary, Sheppard, George S., primary, Wang, Le, primary, Fidanze, Steve, primary, Pratt, John K., primary, Liu, Dachun, primary, Hasvold, Lisa, primary, Uziel, Tamar, primary, Lu, Xin, primary, Kohlhapp, Fred, primary, Fang, Guowei, primary, Elmore, Steven W., primary, Rosenberg, Saul H., primary, McDaniel, Keith F., primary, Kati, Warren M., primary, and Shen, Yu, primary

Published
2023
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31. Opposite effects of neuronal and glial A2A receptors on glutamatergic synapse remodeling during synaptogenesis

Author

Pressey, Jessica, Louboutin, Floriane, Russeau, Marion, Faivre, Emily, Montmasson, Claire, Carvalho, Kervin, Buée, Luc, Blum, David, Lévi, Sabine, Institut du Fer à Moulin (IFM - Inserm U1270 - SU), Institut National de la Santé et de la Recherche Médicale (INSERM)-Sorbonne Université (SU), Lille Neurosciences & Cognition - U 1172 (LilNCog), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Lille-Centre Hospitalier Régional Universitaire [Lille] (CHRU Lille), and FENS

Subjects
[SDV.NEU.NB]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology
Abstract

International audience

Published
2022

32. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Author

Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, Matt T., Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, William J., Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Van Drie, John H., McElligott, David, Kesicki, Ed, Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, and Bromberg, Kenneth D.

Published
2017
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34. Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Author

Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, T. Matt, Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, J. William, Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Kluge, Arthur F., Patane, Michael A., Van Drie, John H., Wang, Ce, McElligott, David, Kesicki, Edward A., Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, and Bromberg, Kenneth D.

Published
2018
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36. Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Author

Zhang, Lu, primary, Cai, Tianyu, additional, Lin, Xiaoyu, additional, Huang, Xiaoli, additional, Bui, Mai H., additional, Plotnik, Joshua P., additional, Bellin, Richard J., additional, Faivre, Emily J., additional, Kuruvilla, Vinitha M., additional, Lam, Lloyd T., additional, Lu, Xin, additional, Zha, Zheng, additional, Feng, Weiguo, additional, Hessler, Paul, additional, Uziel, Tamar, additional, Zhang, Qi, additional, Cavazos, Antonio, additional, Han, Lina, additional, Ferguson, Debra C., additional, Mehta, Gaurav, additional, Shanmugavelandy, Sriram S., additional, Magoc, Terrance J., additional, Rowe, Jenny, additional, Goodwin, Neal C., additional, Dorritie, Kathleen A., additional, Boyiadzis, Michael, additional, Albert, Daniel H., additional, McDaniel, Keith F., additional, Kati, Warren M., additional, Konopleva, Marina, additional, and Shen, Yu, additional

Published
2021
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38. Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Author

Sheppard, George S., primary, Wang, Le, additional, Fidanze, Steven D., additional, Hasvold, Lisa A., additional, Liu, Dachun, additional, Pratt, John K., additional, Park, Chang H., additional, Longenecker, Kenton, additional, Qiu, Wei, additional, Torrent, Maricel, additional, Kovar, Peter J., additional, Bui, Mai, additional, Faivre, Emily, additional, Huang, Xiaoli, additional, Lin, Xiaoyu, additional, Wilcox, Denise, additional, Zhang, Lu, additional, Shen, Yu, additional, Albert, Daniel H., additional, Magoc, Terrance J., additional, Rajaraman, Ganesh, additional, Kati, Warren M., additional, and McDaniel, Keith F., additional

Published
2020
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45. Abstract 4960: First-in-class, highly BDII-selective BET family inhibitor ABBV-744 displays potent anti-tumor activity in androgen receptor positive prostate cancer models and an improved tolerability profile

Author

Faivre, Emily J., primary, Wilcox, Denise, additional, Ha-Bui, Mai, additional, Hessler, Paul, additional, Sehgal, Vasudha, additional, Lu, Xin, additional, Uziel, Tamar, additional, Mehta, Gaurav, additional, Albert, Daniel H., additional, McDaniel, Keith, additional, Kati, Warren, additional, and Shen, Yu, additional

Published
2018
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46. Abstract 800: ABBV-744, a first-in-class and highly selective inhibitor of the second bromodomain of BET family proteins, displays robust activities in preclinical models of acute myelogenous leukemia

Author

Lin, Xiaoyu, primary, Huang, Xiaoli, additional, Bellin, Richard, additional, Faivre, Emily, additional, Hessler, Paul, additional, Lam, Lloyd, additional, Bui, Mai Ha, additional, Wilcox, Denise, additional, Uziel, Tamar, additional, Ferguson, Debra C., additional, Magoc, Terrance J., additional, Albert, Daniel H., additional, McDaniel, Keith F., additional, Kati, Warren, additional, and Shen, Yu, additional

Published
2018
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47. Abstract 931: Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor

Author

Sheppard, George S., primary, Wang, Le, additional, Fidanze, Steven D., additional, Hasvold, Lisa A., additional, Liu, Dachun, additional, Pratt, John K., additional, Park, Chang H., additional, Bui, Mai-Ha, additional, Faivre, Emily J., additional, Huang, Xiaoli, additional, Lin, Xiaoyu, additional, Wilcox, Denise M., additional, Shen, Yu, additional, Albert, Daniel H., additional, Magoc, Terrance J., additional, Rajaraman, Ganesh, additional, Kati, Warren M., additional, and McDaniel, Keith F., additional

Published
2018
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49. Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Author

McDaniel, Keith F., primary, Wang, Le, additional, Soltwedel, Todd, additional, Fidanze, Steven D., additional, Hasvold, Lisa A., additional, Liu, Dachun, additional, Mantei, Robert A., additional, Pratt, John K., additional, Sheppard, George S., additional, Bui, Mai H., additional, Faivre, Emily J., additional, Huang, Xiaoli, additional, Li, Leiming, additional, Lin, Xiaoyu, additional, Wang, Rongqi, additional, Warder, Scott E., additional, Wilcox, Denise, additional, Albert, Daniel H., additional, Magoc, Terrance J., additional, Rajaraman, Ganesh, additional, Park, Chang H., additional, Hutchins, Charles W., additional, Shen, Jianwei J., additional, Edalji, Rohinton P., additional, Sun, Chaohong C., additional, Martin, Ruth, additional, Gao, Wenqing, additional, Wong, Shekman, additional, Fang, Guowei, additional, Elmore, Steven W., additional, Shen, Yu, additional, and Kati, Warren M., additional

Published
2017
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50. Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Author

Lam, Lloyd T., primary, Lin, Xiaoyu, additional, Faivre, Emily J., additional, Yang, Ziping, additional, Huang, Xiaoli, additional, Wilcox, Denise M., additional, Bellin, Richard J., additional, Jin, Sha, additional, Tahir, Stephen K., additional, Mitten, Michael, additional, Magoc, Terry, additional, Bhathena, Anahita, additional, Kati, Warren M., additional, Albert, Daniel H., additional, Shen, Yu, additional, and Uziel, Tamar, additional

Published
2017
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