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15 results on '"Lisa Hasvold"'

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

Author

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

Abstract

High level of concomitant Bim and Bcl-2 expression correlates with sensitivity to ABBV-075-induced apoptosis

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

Author

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

Abstract

Apoptosis induction by MS417 across cancer cell lines

Published
2023
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3. Supplemental figure 13 from Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Author

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

Abstract

Restoration of Myc expression under BET inhibitor treatment failed to rescue cells from apoptosis or cell cycle arrest

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

Author

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

Abstract

ABBV-075 is a potent and selective BET family bromodomain inhibitor that recently entered phase I clinical trials. Comprehensive preclinical characterization of ABBV-075 demonstrated broad activity across cell lines and tumor models, representing a variety of hematologic malignancies and solid tumor indications. In most cancer cell lines derived from solid tumors, ABBV-075 triggers prominent G1 cell-cycle arrest without extensive apoptosis. In this study, we show that ABBV-075 efficiently triggers apoptosis in acute myeloid leukemia (AML), non-Hodgkin lymphoma, and multiple myeloma cells. Apoptosis induced by ABBV-075 was mediated in part by modulation of the intrinsic apoptotic pathway, exhibiting synergy with the BCL-2 inhibitor venetoclax in preclinical models of AML. In germinal center diffuse large B-cell lymphoma, BCL-2 levels or venetoclax sensitivity predicted the apoptotic response to ABBV-075 treatment. In vivo combination studies uncovered surprising benefits of low doses of ABBV-075 coupled with bortezomib and azacitidine treatment, despite the lack of in vitro synergy between ABBV-075 and these agents. The in vitro/in vivo activities of ABBV-075 described here may serve as a useful reference to guide the development of ABBV-075 and other BET family inhibitors for cancer therapy. Cancer Res; 77(11); 2976–89. ©2017 AACR.

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

Author

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

Abstract

ABBV-075 inhibits Bcl-XL transcription and displace BRD4 from Bcl-XL regulatory regions

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

Author

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

Abstract

Apoptosis induction by ABBV-075 across cancer cell lines

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

Author

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

Abstract

Induction of apoptosis across cancer cell lines and CD34 normal cells

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

Author

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

Abstract

Anti-proliferative activity of ABBV-075 across cancer cell lines

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

Author

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

Abstract

BET inhibitor causes cell cycle arrest and triggers senescence in solid tumor cells

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

Author

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

Abstract

supplemental figure legends

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

Author

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

Abstract

Expression of exogenous Bcl-XL rescues ABBV-075 induced apoptosis but not cell cycle arrest

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

Author

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

Abstract

Down regulation of Bcl-XL by MS417 and ABBV-075

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

Author

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

Abstract

ABBV-075 inhibits genes that are important for cell cycle

Published
2023
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14. Synthesis and structure-activity relationships of 2-pyridones: a novel series of potent DNA gyrase inhibitors as antibacterial agents

Author

Qun Li, Daniel T. W. Chu, Akiyo Claiborne, Curt S. Cooper, Cheuk M. Lee, Kathleen Raye, Kristine B. Berst, Pamela Donner, Weibo Wang, Lisa Hasvold, Anthony Fung, Zhenkun Ma, Michael Tufano, Robert Flamm, Linus L. Shen, John Baranowski, Angela Nilius, Jeff Alder, Jonathan Meulbroek, Kennan Marsh, DeAnne Crowell, Yuhua Hui, Louis Seif, Laura M. Melcher, Rodger Henry, Steven Spanton, Ramin Faghih, Larry L. Klein, S. Ken Tanaka, and Jacob J. Plattner

Subjects
DNA, Bacterial, Models, Molecular, Magnetic Resonance Spectroscopy, Pyrimidine, Stereochemistry, Pyridones, Microbial Sensitivity Tests, Crystallography, X-Ray, Gram-Positive Bacteria, Chemical synthesis, DNA gyrase, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Gram-Negative Bacteria, Animals, Topoisomerase II Inhibitors, Enzyme Inhibitors, Antibacterial agent, Bicyclic molecule, Bacteria, Molecular Structure, Chemistry, Quinolizine, Drug Resistance, Microbial, Anti-Bacterial Agents, Rats, DNA Topoisomerases, Type II, Solubility, Lactam, Molecular Medicine, Antibacterial activity, Quinolizines
Abstract

Two novel series of 2-pyridones were synthesized by transposition of the nitrogen of 4-quinolones to the bridgehead position. This subtle interchange of the nitrogen atom with a carbon atom yielded two novel heterocyclic nuclei, pyrido[1,2-alpha]pyrimidine and quinolizine, which had not previously been evaluated as antibacterial agents and were found to be potent inhibitors of DNA gyrase. Quinolizines with a methyl group at the 9-position such as (S)-45a (ABT-719) demonstrate exceptional broad spectrum antibacterial activity. Most notably, they are active against resistant bacteria such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant strains of enterococci, and ciprofloxacin-resistant organisms. In addition, 2-pyridones also possess favorable physiochemical and pharmacokinetic properties. These 2-pyridones were synthesized from the commercially available starting materials by 10-17 linear transformations. The structure of an adduct yielded by this sequence, (S)-45a (ABT-719), was determined by X-ray crystallographic analysis.

Published
1996

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