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Journal Articles

Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) Exert Potent Single Agent and Synergistic Activity with Ibrutinib and Venetoclax Against Human Mantle Cell Lymphoma Cells

Baohua Sun, MD PhD, Warren Fiskus, PhD, Liang Zhang, MD PhD, Kanak Raina, PhD, Kevin Coleman, PhD, Jim Winkler, PhD, Yimin Qian, PhD, Andrew Crew, PhD, Angela Shen, MD, Dyana T Saenz, PhD, Christopher P Mill, PhD, Michael Wang, MD, Craig Crews, PhD, Kapil N. Bhalla, MD

Blood (2016) 128 (22): 1058.

https://doi.org/10.1182/blood.V128.22.1058.1058

Published: 2016

Journal Articles

Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells

Dyana T Saenz, PhD, Warren Fiskus, PhD, Kanak Raina, PhD, Taghi Manshouri, PhD, Kevin Coleman, PhD, Jim Winkler, PhD, Yimin Qian, PhD, Andrew Crew, PhD, Angela Shen, MD, Christopher P Mill, PhD, Baohua Sun, MD PhD, Srdan Verstovsek, MD PhD, Craig Crews, PhD, Kapil N. Bhalla, MD

Blood (2016) 128 (22): 747.

https://doi.org/10.1182/blood.V128.22.747.747

Published: 2016

Journal Articles

Superior Activity of BET Protein Bromodomain Antagonist-Based Combination with JAK Kinase, PIM Kinase or Heat Shock Protein 90 Inhibitor Against Post-MPN-MF sAML Cells

Dyana T Saenz, Warren Fiskus, PhD, Taghi Manshouri, PhD, Baohua Sun, MD PhD, Stephanie Krieger, Simrit Parmar, MD, Srdan Verstovsek, MD PhD, Kapil N. Bhalla, MD

Blood (2015) 126 (23): 1269.

https://doi.org/10.1182/blood.V126.23.1269.1269

Published: 2015

Journal Articles

BET Protein Bromodomain Antagonist-Based Combinations Exert Synergistic Pre-Clinical Activity Against Ibrutinib-Sensitive or -Resistant Human Mantle Cell Lymphoma (MCL) Cells

Baohua Sun, MD PhD, Warren Fiskus, PhD, Dyana T Saenz, Stephanie Krieger, Liang Zhang, MD PhD, Simrit Parmar, MD, Michael Wang, MD, Kapil N. Bhalla, MD

Blood (2015) 126 (23): 3704.

https://doi.org/10.1182/blood.V126.23.3704.3704

Published: 2015

Journal Articles

Mechanistic Role of HEXIM1 Induction in BRD4-Antagonist Mediated Growth Inhibition, Differentiation and in Vivo Lethal Activity Against Human AML Blast Progenitor Cells

Santhana G. T. Devaraj, PhD, Warren Fiskus, PhD, Bhavin Shah, Sunil Sharma, Jun Qi, PhD, Baohua Sun, MD PhD, Saikat Saha, PhD, Swaminathan Padmanabhan Iyer, MD, Youli Zu, MD PhD, James Bradner, MD, Kapil N. Bhalla, MD

Blood (2014) 124 (21): 3534.

https://doi.org/10.1182/blood.V124.21.3534.3534

Published: 2014

Journal Articles

Combined Targeting of β-Catenin and FLT-3 Is Synergistically Lethal Against Cultured and Primary AML Blast Progenitor Cells Expressing FLT3 Internal Tandem Duplication (ITD)

Saikat Saha, PhD, Warren Fiskus, PhD, Sunil Sharma, Bhavin Shah, Anna T Rogojina, Santhana G. T. Devaraj, PhD, Baohua Sun, MD PhD, Christopher Leveque, MD, Youli Zu, MD PhD, Swaminathan Padmanabhan Iyer, MD, Kapil N. Bhalla, MD

Blood (2014) 124 (21): 618.

https://doi.org/10.1182/blood.V124.21.618.618

Published: 2014

Journal Articles

Superior Pre-Clinical Activity of BET (Bromodomain and Extra terminal) Protein Antagonist Combined with Ibrutinib, Panobinostat or Carfilzomib Against Human Mantle Cell Lymphoma (MCL) Cells

Baohua Sun, MD PhD, Warren Fiskus, PhD, Bhavin Shah, Jun Qi, PhD, Santhana G. T. Devaraj, PhD, Swaminathan Padmanabhan Iyer, MD, Sunil Sharma, James Bradner, MD, Youli Zu, MD PhD, Kapil N. Bhalla, MD

Blood (2014) 124 (21): 918.

https://doi.org/10.1182/blood.V124.21.918.918

Published: 2014

Journal Articles

Combined Targeting of Chromatin Modifying Enzymes LSD1, EZH2 and Histone Deacetylases (HDACs) Has Superior Efficacy Against Human Mantle Cell Lymphoma Cells

Warren Fiskus, PhD, Sunil Sharma, MD, Rekha Rao, PhD, Ramesh Balusu, PhD, Sreedhar Venkannagari, PhD, Stacey Hembruff, MS, Siddhartha Ganguly, MD, Eduardo M. Sotomayor, Jianguo Tao, MD, PhD, David J. Bearss, PhD, Kapil N. Bhalla, MD

Blood (2011) 118 (21): 2429.

https://doi.org/10.1182/blood.V118.21.2429.2429

Published: 2011

Journal Articles

Treatment with β-Catenin Antagonist BC2059 Exerts Single Agent Efficacy and Exerts Improved Activity with Tyrosine Kinase Inhibitor (TKI) or Pan-Histone Deacetylase (HDAC) Inhibitor Against Human CML and Myeloproliferative Neoplasm (MPN) Progenitor Cells

Warren Fiskus, PhD, Jacqueline Smith, MS, Uma Mudunuru, MS, Stacey Hembruff, MS, Ruben Reyes, MD, Sunil Abhyankar, MD, Joseph McGuirk, DO, Omar S. Aljitawi, MD, Siddhartha Ganguly, MD, Stephen K. Horrigan, PhD, Sunil Sharma, MD, Kapil N. Bhalla, MD

Blood (2011) 118 (21): 65.

https://doi.org/10.1182/blood.V118.21.65.65

Published: 2011

Journal Articles

A Phase II Trial of Panobinostat, an Orally Available Deacetylase Inhibitor (DACi), in Patients with Primary Myelofibrosis (PMF), Post Essential Thrombocythemia (ET), and Post Polycythemia Vera (PV) Myelofibrosis

Daniel J DeAngelo, MD, PhD, Ayalew Tefferi, MD, Warren Fiskus, PhD, Ruben A. Mesa, MD, Carole S. Paley, MD, Martha Wadleigh, MD, David S. Snyder, MD, Kebede Begna, MD, Michael S. Ondovik, Jessica Rine, Kapil N. Bhalla, MD

Blood (2010) 116 (21): 630.

https://doi.org/10.1182/blood.V116.21.630.630

Published: 2010

Journal Articles

Pan-Histone Deacetylase (HDAC) Inhibitor LBH589 Depletes CXCR4 Levels and Signaling, Exerting Synergistic Anti-Leukemia Activity in Combination with CXCR4 Antagonists.

Aditya Mandawat, BS, Warren Fiskus, PhD, Andrea Jakubowski, Rekha Rao, PhD, Zixuan Wang, PhD, Pravina Fernandez, MS, Yongchao Wang, MS, Pearl Lee, BS, Anand Jillela, MD, Peter Atadja, PhD, Nobutaka Fujii, PhD, Stephen C. Peiper, MD, Kapil Bhalla, MD

Blood (2007) 110 (11): 537.

https://doi.org/10.1182/blood.V110.11.537.537

Published: 2007

Journal Articles

Targeting Histone Deacetylases and Unfolded Protein Mediated Endoplasmic Reticulum (ER) Stress as a Strategy Against Human Mantle Cell Lymphoma.

Rekha Rao, PhD, Warren Fiskus, PhD, Rajeshree Joshi, BS, Jianguang Chen, PhD, Pravina Fernandez, MS, Yongchao Wang, MS, Pearl Lee, BS, Anand Jillella, MD, Jianguo Tao, MD, Peter Atadja, PhD, Eduardo Sotomayor, MD, Kapil Bhalla, MD

Blood (2007) 110 (11): 1378.

https://doi.org/10.1182/blood.V110.11.1378.1378

Published: 2007

Journal Articles

Molecular Characterization and Drug-Sensitivity of Pan Histone Deacetylase Inhibitor Resistant Human Acute Myeloid Leukemia Cells.

Warren Fiskus, PhD, Rekha Rao, PhD, Pravina Fernandez, MS, Bryan Herger, PhD, Yonghua Yang, PhD, Jianguang Chen, PhD, Yongchao Wang, MS, Aditya Mandawat, BS, Pearl Lee, BS, Peter Atadja, PhD, Kapil Bhalla, MD

Blood (2007) 110 (11): 807.

https://doi.org/10.1182/blood.V110.11.807.807

Published: 2007

Journal Articles

Inhibition of Histone Deacetylase (HDAC) 6 and/or Heat Shock Protein (HSP) 90: A Strategy To Abrogate Multi-Level Protective Responses to Misfolded Proteins Induced by Proteasome Inhibitors in Human Leukemia Cells.

Rekha Rao, PhD, Warren Fiskus, PhD, Bryan Herger, PhD, Peter Atadja, PhD, Kapil Bhalla, MD

Blood (2006) 108 (11): 257.

https://doi.org/10.1182/blood.V108.11.257.257

Published: 2006

Journal Articles

Hydroxamate Pan-HDAC Inhibitor LBH589 Depletes EZH2 and DNMT1, Partly through hsp90 Inhibition and Its Chaperone Association with DNMT1.

Warren Fiskus, PhD, Bryan Herger, Ph.D., Rekha Rao, Ph.D., Peter Atadja, Kapil Bhalla, M.D.

Blood (2006) 108 (11): 2233.

https://doi.org/10.1182/blood.V108.11.2233.2233

Published: 2006

Journal Articles

Treatment with the Heat Shock Protein (hsp) 90 Inhibitor17-Dimethylaminoethylamino-17-Demethoxygeldanamycin (DMAG) Abrogates the Levels and Activity of the Receptor Tyrosine Kinase TrkA in Acute Leukemia Cells.

Sandhya Kumaraswamy, PhD, Que T. Lambert, MS, Kathy Rocha, BS, Purva Bali, MS, Warren Fiskus, PhD, Maria Balasis, BS, Michael Pranpat, MS, Sandhya Boyapalle, PhD, Alison Hannah, MD, Gary W. Reuther, PhD, Kapil Bhalla, MD

Blood (2005) 106 (11): 4401.

https://doi.org/10.1182/blood.V106.11.4401.4401

Published: 2005

Journal Articles

Co-Treatment with a Novel Heat Shock Protein (hsp) 90 Inhibitor IPI504 and the Histone Deacetylase Inhibitor (HDI) Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA): A Highly Active Combination Against Wild Type or Mutant Bcr-Abl-T315I or FLT-3-ITD-Containing Human Leukemia Cells.

Warren Fiskus, PhD, Purva Bali, MS, Michael Pranpat, MS, Maria Balasis, BS, Sandhya Kumaraswamy, PhD, Sandhya Boyapalle, PhD, Kathy Rocha, BS, Jeffery Tong, MD, Victoria Richon, PhD, Emmanuel Normant, PhD, Kapil Bhalla, MD

Blood (2005) 106 (11): 4461.

https://doi.org/10.1182/blood.V106.11.4461.4461

Published: 2005

Journal Articles

Co-Treatment with the hsp90 Inhibitor 17-Dimethylaminoethylamino-17-Demethoxygeldanamycin (DMAG) and Histone Deacetylase Inhibitor (HDI) Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA): A Highly Active Combination Against Human Mantle Cell Lymphoma (MCL) Cells.

Angela Hatter, BS, Purva Bali, MS, Maria Balasis, BS, Warren Fiskus, PhD, Sandhya Boyapalle, PhD, Sandhya Kumaraswamy, PhD, Kathy Rocha, BS, Michael Pranpat, BS, Alison Hannah, MD, Eduardo Sotomayor, MD, PhD, Victoria Richon, PhD, Kapil Bhalla, MD

Blood (2005) 106 (11): 2418.

https://doi.org/10.1182/blood.V106.11.2418.2418

Published: 2005

Journal Articles

Histone Deacetylase Inhibitors LBH589 and LAQ824 Deplete Ezh2 and Associated Polycomb Repressive Complex 2/3 Proteins Resulting in Downregulation of HOXA9 and MEIS1 Expression in Human Acute Leukemia Cells.

Warren Fiskus, PhD, Michael Pranpat, MS, Purva Bali, MS, Sandhya Kumaraswamy, PhD, Sandhya Boyapalle, PhD, Kathy Rocha, BS, Maria Balasis, BS, Peter Atadja, PhD, Kapil Bhalla, MD

Blood (2005) 106 (11): 2482.

https://doi.org/10.1182/blood.V106.11.2482.2482

Published: 2005

Journal Articles

Increased Levels of the Heat Shock Protein (hsp) 70 Contribute as a Pro-Survival and Pro-Growth Mechanism in the Transformation of Bone Marrow Progenitor Cells.

Sandhya Boyapalle, PhD, Kathy Rocha, BS, Fei Guo, PhD, Purva Bali, MS, Maria Balasis, BS, Warren Fiskus, PhD, Sandhya Kumaraswamy, PhD, Michael Pranpat, MS, Kapil Bhalla, MD

Blood (2005) 106 (11): 1374.

https://doi.org/10.1182/blood.V106.11.1374.1374

Published: 2005

NARROW

Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) Exert Potent Single Agent and Synergistic Activity with Ibrutinib and Venetoclax Against Human Mantle Cell Lymphoma Cells

Superior Lethal Activity of Novel BET Protein Proteolysis Targeting Chimera (BETP-PROTACs) Versus Betp Bromodomain Inhibitor (BETi) Against Post-Myeloproliferative Neoplasm (MPN) Secondary (s) AML Cells

Superior Activity of BET Protein Bromodomain Antagonist-Based Combination with JAK Kinase, PIM Kinase or Heat Shock Protein 90 Inhibitor Against Post-MPN-MF sAML Cells

BET Protein Bromodomain Antagonist-Based Combinations Exert Synergistic Pre-Clinical Activity Against Ibrutinib-Sensitive or -Resistant Human Mantle Cell Lymphoma (MCL) Cells

Mechanistic Role of HEXIM1 Induction in BRD4-Antagonist Mediated Growth Inhibition, Differentiation and in Vivo Lethal Activity Against Human AML Blast Progenitor Cells

Combined Targeting of β-Catenin and FLT-3 Is Synergistically Lethal Against Cultured and Primary AML Blast Progenitor Cells Expressing FLT3 Internal Tandem Duplication (ITD)

Superior Pre-Clinical Activity of BET (Bromodomain and Extra terminal) Protein Antagonist Combined with Ibrutinib, Panobinostat or Carfilzomib Against Human Mantle Cell Lymphoma (MCL) Cells

Combined Targeting of Chromatin Modifying Enzymes LSD1, EZH2 and Histone Deacetylases (HDACs) Has Superior Efficacy Against Human Mantle Cell Lymphoma Cells

Treatment with β-Catenin Antagonist BC2059 Exerts Single Agent Efficacy and Exerts Improved Activity with Tyrosine Kinase Inhibitor (TKI) or Pan-Histone Deacetylase (HDAC) Inhibitor Against Human CML and Myeloproliferative Neoplasm (MPN) Progenitor Cells

A Phase II Trial of Panobinostat, an Orally Available Deacetylase Inhibitor (DACi), in Patients with Primary Myelofibrosis (PMF), Post Essential Thrombocythemia (ET), and Post Polycythemia Vera (PV) Myelofibrosis

Pan-Histone Deacetylase (HDAC) Inhibitor LBH589 Depletes CXCR4 Levels and Signaling, Exerting Synergistic Anti-Leukemia Activity in Combination with CXCR4 Antagonists.

Targeting Histone Deacetylases and Unfolded Protein Mediated Endoplasmic Reticulum (ER) Stress as a Strategy Against Human Mantle Cell Lymphoma.

Molecular Characterization and Drug-Sensitivity of Pan Histone Deacetylase Inhibitor Resistant Human Acute Myeloid Leukemia Cells.

Inhibition of Histone Deacetylase (HDAC) 6 and/or Heat Shock Protein (HSP) 90: A Strategy To Abrogate Multi-Level Protective Responses to Misfolded Proteins Induced by Proteasome Inhibitors in Human Leukemia Cells.

Hydroxamate Pan-HDAC Inhibitor LBH589 Depletes EZH2 and DNMT1, Partly through hsp90 Inhibition and Its Chaperone Association with DNMT1.

Treatment with the Heat Shock Protein (hsp) 90 Inhibitor17-Dimethylaminoethylamino-17-Demethoxygeldanamycin (DMAG) Abrogates the Levels and Activity of the Receptor Tyrosine Kinase TrkA in Acute Leukemia Cells.

Co-Treatment with a Novel Heat Shock Protein (hsp) 90 Inhibitor IPI504 and the Histone Deacetylase Inhibitor (HDI) Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA): A Highly Active Combination Against Wild Type or Mutant Bcr-Abl-T315I or FLT-3-ITD-Containing Human Leukemia Cells.

Co-Treatment with the hsp90 Inhibitor 17-Dimethylaminoethylamino-17-Demethoxygeldanamycin (DMAG) and Histone Deacetylase Inhibitor (HDI) Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA): A Highly Active Combination Against Human Mantle Cell Lymphoma (MCL) Cells.

Histone Deacetylase Inhibitors LBH589 and LAQ824 Deplete Ezh2 and Associated Polycomb Repressive Complex 2/3 Proteins Resulting in Downregulation of HOXA9 and MEIS1 Expression in Human Acute Leukemia Cells.

Increased Levels of the Heat Shock Protein (hsp) 70 Contribute as a Pro-Survival and Pro-Growth Mechanism in the Transformation of Bone Marrow Progenitor Cells.

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American Society of Hematology

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American Society of Hematology

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