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1. BID expression determines the apoptotic fate of cancer cells after abrogation of the spindle assembly checkpoint by AURKB or TTK inhibitors

Author

Bertran-Alamillo, Jordi, Giménez-Capitán, Ana, Román, Ruth, Talbot, Sara, Whiteley, Rebecca, Floc’h, Nicolas, Martínez-Pérez, Elizabeth, Martin, Matthew J., Smith, Paul D., Sullivan, Ivana, Terp, Mikkel G., Saeh, Jamal, Marino-Buslje, Cristina, Fabbri, Giulia, Guo, Grace, Xu, Man, Tornador, Cristian, Aguilar-Hernández, Andrés, Reguart, Noemí, Ditzel, Henrik J., Martínez-Bueno, Alejandro, Nabau-Moretó, Núria, Gascó, Amaya, Rosell, Rafael, Pease, J. Elizabeth, Polanska, Urszula M., Travers, Jon, Urosevic, Jelena, and Molina-Vila, Miguel A.

Published
2023
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2. Supplementary Figure 1 from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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3. Data from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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4. Supplementary Figure 3 from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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5. Supplementary Figure 2 from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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6. Supplementary Data 1 from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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7. Supplementary Figure 4 from Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, primary, Della Corte, Carminia M., primary, Stewart, C. Allison, primary, Wang, Qi, primary, Shen, Li, primary, Cardnell, Robert J., primary, Wang, Jing, primary, Polanska, Urszula M., primary, Andersen, Courtney, primary, Saeh, Jamal, primary, Pease, J. Elizabeth, primary, Travers, Jon, primary, Fabbri, Giulia, primary, Gay, Carl M., primary, Urosevic, Jelena, primary, and Byers, Lauren A., primary

Published
2023
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8. Targeting BCL2 Overcomes Resistance and Augments Response to Aurora Kinase B Inhibition by AZD2811 in Small Cell Lung Cancer

Author

Ramkumar, Kavya, primary, Tanimoto, Azusa, additional, Della Corte, Carminia M., additional, Stewart, C. Allison, additional, Wang, Qi, additional, Shen, Li, additional, Cardnell, Robert J., additional, Wang, Jing, additional, Polanska, Urszula M., additional, Andersen, Courtney, additional, Saeh, Jamal, additional, Pease, J. Elizabeth, additional, Travers, Jon, additional, Fabbri, Giulia, additional, Gay, Carl M., additional, Urosevic, Jelena, additional, and Byers, Lauren A., additional

Published
2023
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9. Supplementary Figure 2 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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10. Supplementary Figure 1 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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11. Supplementary Table 2 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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12. Supplementary Figure 5 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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13. Supplementary Figure Legends from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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14. Data from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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15. Supplementary Figure 4 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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16. Supplementary Figure 3 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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17. Supplementary Table 3 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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18. Supplementary Figure 6 from AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., primary, Robinson, David, primary, Sandin, Linda C., primary, Delpuech, Oona, primary, Zhang, Pei, primary, Hanson, Lyndsey, primary, Farrington, Paul, primary, Bell, Sigourney, primary, Falenta, Katarzyna, primary, Gibbons, Francis D., primary, Lindsay, Nicola, primary, Smith, Aaron, primary, Wilson, Joanne, primary, Roberts, Karen, primary, Tonge, Michael, primary, Hopcroft, Philip, primary, Willis, Sophie E., primary, Roudier, Martine P., primary, Rooney, Claire, primary, Coker, Elizabeth A., primary, Jaaks, Patricia, primary, Garnett, Mathew J., primary, Fawell, Stephen E., primary, Jones, Clifford D., primary, Ward, Richard A., primary, Simpson, Iain, primary, Cosulich, Sabina C., primary, Pease, J. Elizabeth, primary, and Smith, Paul D., primary

Published
2023
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20. Abstract P2-13-18: Activity and tolerability of combination of trastuzumab deruxtecan with olaparib in preclinical HER2+ and HER2-low breast cancer models

Author

Proia, Theresa, primary, Wallez, Yann, additional, Bashi, Azadeh Cheraghchi, additional, Wilson, Zena, additional, Randle, Suzanne, additional, Anderton, Mark, additional, Carroll, Danielle, additional, Rasheed, Zeshaan, additional, Pease, J. Elizabeth, additional, Leo, Elisabetta, additional, and Mettetal, Jerome, additional

Published
2022
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21. Abstract P2-13-23: Activity and tolerability of combination of trastuzumab deruxtecan with the pan-AKT inhibitor capivasertib in preclinical HER2+ and HER2-low breast cancer models

Author

Bashi, Azadeh Cheraghchi, primary, Proia, Theresa, additional, Randle, Suzanne, additional, Anderton, Mark, additional, Rasheed, Zeshaan, additional, Pease, J. Elizabeth, additional, Barry, Simon, additional, Carroll, Danielle, additional, and Mettetal, Jerome, additional

Published
2022
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22. A phase 1/2 study of the combination of acalabrutinib and vistusertib in patients with relapsed/refractory B-cell malignancies

Author

Collins, Graham P., primary, Clevenger, Tracy N., additional, Burke, Kathleen A., additional, Yang, Buyue, additional, MacDonald, Alex, additional, Cunningham, David, additional, Fox, Christopher P., additional, Goy, Andre, additional, Gribben, John, additional, Nowakowski, Grzegorz S., additional, Roschewski, Mark, additional, Vose, Julie M., additional, Vallurupalli, Anusha, additional, Cheung, Jean, additional, Raymond, Amelia, additional, Nuttall, Barrett, additional, Stetson, Dan, additional, Dougherty, Brian A., additional, Schalkwijk, Stein, additional, Carnevalli, Larissa S., additional, Willis, Brandon, additional, Tao, Lin, additional, Harrington, Elizabeth A., additional, Hamdy, Ahmed, additional, Izumi, Raquel, additional, Pease, J. Elizabeth, additional, Frigault, Melanie M., additional, and Flinn, Ian, additional

Published
2021
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23. Abstract 1107: Precision phosphoproteomic analysis in Chr22q11.2 amplified NSCLC cells reveals distinct signaling corruption and response to Aurora kinase B inhibition

Author

Dokal, Arran, primary, Bertran-Alamillo, Jordi, additional, Wilkes, Edmund, additional, Lewis, Hilary, additional, Gimenez-Capitan, Ana, additional, Greenhalgh, Calum, additional, Osuntola, Ruth, additional, Higazi-Vega, Maruan, additional, Ellison, Shona, additional, Rajeeve, Vinothini, additional, Fabbri, Giulia, additional, Polanska, Urszula, additional, Pease, J. Elizabeth, additional, Rodriguez-Cutillas, Pedro, additional, Urosevic, Jelena, additional, Molina-Vila, Miguel Angel, additional, Britton, David, additional, and Travers, Jon, additional

Published
2021
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24. AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib

Author

Flemington, Vikki, primary, Davies, Emma J., additional, Robinson, David, additional, Sandin, Linda C., additional, Delpuech, Oona, additional, Zhang, Pei, additional, Hanson, Lyndsey, additional, Farrington, Paul, additional, Bell, Sigourney, additional, Falenta, Katarzyna, additional, Gibbons, Francis D., additional, Lindsay, Nicola, additional, Smith, Aaron, additional, Wilson, Joanne, additional, Roberts, Karen, additional, Tonge, Michael, additional, Hopcroft, Philip, additional, Willis, Sophie E., additional, Roudier, Martine P., additional, Rooney, Claire, additional, Coker, Elizabeth A., additional, Jaaks, Patricia, additional, Garnett, Mathew J., additional, Fawell, Stephen E., additional, Jones, Clifford D., additional, Ward, Richard A., additional, Simpson, Iain, additional, Cosulich, Sabina C., additional, Pease, J. Elizabeth, additional, and Smith, Paul D., additional

Published
2020
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25. A Phase I/II Study of AZD2811 Nanoparticles (NP) As Monotherapy or in Combination in Treatment-Naïve or Relapsed/Refractory AML/MDS Patients Not Eligible for Intensive Induction Therapy

Author

Donnellan, William B., primary, Atallah, Ehab L., additional, Asch, Adam S., additional, Patel, Manish R., additional, Yang, Jay, additional, Eghtedar, Alireza, additional, Borthakur, Gautam M., additional, Charlton, Julie, additional, MacDonald, Alexander, additional, Korzeniowska, Anna, additional, Sainsbury, Elizabeth, additional, Strickland, Donald K., additional, Jones, Suzanne, additional, Overend, Philip, additional, Adelman, Carrie A., additional, Fabbri, Giulia, additional, Travers, Jon, additional, Smith, Simon, additional, Pease, J. Elizabeth, additional, and Cosaert, Jan, additional

Published
2019
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28. A Phase I/II, Open-Label, Multicentre 2-Part Study to Assess the Safety, Tolerability, Pharmacokinetics, and Efficacy of AZD2811 Nanoparticle As Monotherapy or in Combination in Treatment-Naïve or Relapsed/Refractory Acute Myeloid Leukaemia/Myelodysplastic Syndrome Patients Not Eligible for Intensive Induction Therapy

Author

Donnellan, William B., primary, Atallah, Ehab L., additional, Asch, Adam S., additional, Patel, Manish R, additional, Charlton, Julie, additional, MacDonald, Alexander, additional, Young, Elena, additional, Sainsbury, Elizabeth, additional, Strickland, Donald, additional, Jones, Suzanne, additional, Overend, Philip, additional, Adelman, Carrie A., additional, Travers, Jon, additional, Smith, Simon, additional, Pease, J. Elizabeth, additional, and Brugger, Wolfram, additional

Published
2018
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29. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265PDiffuse Large B-Cell Lymphoma

Author

Scott, James S., Degorce, Sébastien L., Anjum, Rana, Culshaw, Janet, Davies, Robert D. M., Davies, Nichola L., Dillman, Keith S., Dowling, James E., Drew, Lisa, Ferguson, Andrew D., Groombridge, Sam D., Halsall, Christopher T., Hudson, Julian A., Lamont, Scott, Lindsay, Nicola A., Marden, Stacey K., Mayo, Michele F., Pease, J. Elizabeth, Perkins, David R., Pink, Jennifer H., Robb, Graeme R., Rosen, Alan, Shen, Minhui, McWhirter, Claire, and Wu, Dedong

Abstract

Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize our scaffold. Compound 28demonstrated a favorable physicochemical and kinase selectivity profile and was identified as a promising in vivo tool with which to explore the role of IRAK4 inhibition in the treatment of mutant MYD88L265Pdiffuse large B-cell lymphoma (DLBCL). Compound 28was shown to be capable of demonstrating inhibition of NF-κB activation and growth of the ABC subtype of DLBCL cell lines in vitro at high concentrations but showed greater effects in combination with a BTK inhibitor at lower concentrations. In vivo, the combination of compound 28and ibrutinib led to tumor regression in an ABC-DLBCL mouse model.

Published
2024
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30. Abstract 1647: Discovery of AZD0364, a potent and selective oral inhibitor of ERK1/2 that is efficacious in both monotherapy and combination therapy in models of NSCLC

Author

Simpson, Iain, primary, Anderton, Mark J., additional, Andrews, David M., additional, Breed, Jason, additional, Davies, Emma, additional, Debreczeni, Judit E., additional, Flemington, Vikki, additional, Gibbons, Francis D., additional, Graham, Mark A., additional, Hopcroft, Philip, additional, Howard, Tina, additional, Hudson, Julian, additional, Jones, Clifford D., additional, Jones, Christopher, additional, Lindsay, Nicola, additional, Pease, J Elizabeth, additional, Rawlins, Philip, additional, Roberts, Karen, additional, Swallow, Steve, additional, St-Gallay, Steve, additional, Tonge, Michael E., additional, and Ward, Richard A., additional

Published
2018
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32. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma

Author

Scott, James S., primary, Degorce, Sébastien L., additional, Anjum, Rana, additional, Culshaw, Janet, additional, Davies, Robert D. M., additional, Davies, Nichola L., additional, Dillman, Keith S., additional, Dowling, James E., additional, Drew, Lisa, additional, Ferguson, Andrew D., additional, Groombridge, Sam D., additional, Halsall, Christopher T., additional, Hudson, Julian A., additional, Lamont, Scott, additional, Lindsay, Nicola A., additional, Marden, Stacey K., additional, Mayo, Michele F., additional, Pease, J. Elizabeth, additional, Perkins, David R., additional, Pink, Jennifer H., additional, Robb, Graeme R., additional, Rosen, Alan, additional, Shen, Minhui, additional, McWhirter, Claire, additional, and Wu, Dedong, additional

Published
2017
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33. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.

Author

Scott, James S., Degorce, Sébastien L., Davies, Nichola L., Lamont, Scott, Lindsay, Nicola A., Pease, J. Elizabeth, Robb, Graeme R., McWhirter, Claire, Anjum, Rana, Dillman, Keith S., Dowling, James E., Drew, Lisa, Ferguson, Andrew D., Mayo, Michele F., Rosen, Alan, Minhui Shen, Culshaw, Janet, Davies, Robert D. M., Groombridge, Sam D., and Halsall, Christopher T.

Published
2017
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34. Preclinical and Early Phase 1 Clinical Data of AZD2811 Nanoparticle in AML, an Aurora B Kinase Inhibitor

Author

Brugger, Wolfram, Ashton, Susan, Adelman, Carrie A., Floc'h, Nicolas, Taylor, Paula, Hattersley, Maureen, Wen, Shenghua, Maratea, Kimberly, Overend, Philip, Fox, Steven, Charlton, Julie, Barry, Simon T, Strickland, Donald, Jones, Suzanne, Burris, Howard A., Greenlees, Carol, MacDonald, Alexander, Pease, J. Elizabeth, and Donnellan, William

Published
2017
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35. Preclinical and Clinical Pharmacodynamics of Pan-Pim Inhibition By AZD1208 in Acute Myeloid Leukemia: Assessment of Pim Isoform Dependency for Bad and 4EBP1 Phosphorylation

Author

McEachern, Kristen A, primary, Tron, Adriana E, additional, O'Connor, Greg, additional, DuPont, Rachel, additional, Gibbons, Francis D, additional, Pablo, Lourdes, additional, Vishwanathan, Karthick, additional, McCoon, Patricia, additional, Cortes, Jorge E., additional, DeAngelo, Daniel J., additional, Minden, Mark D, additional, Uy, Geoffrey L., additional, Neumann, Frank, additional, Keating, Karen, additional, Huszar, Dennis, additional, Pease, J. Elizabeth, additional, Brown, Jeffrey, additional, and Barrett, J. Carl, additional

Published
2014
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36. Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: Synthesis and structure–activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors

Author

Hennequin, Laurent F.A., primary, Ballard, Peter, additional, Boyle, F. Tom, additional, Delouvrié, Bénédicte, additional, Ellston, Rebecca P.A., additional, Halsall, Chris T., additional, Harris, Craig S., additional, Hudson, Kevin, additional, Kendrew, Jane, additional, Pease, J. Elizabeth, additional, Ross, Helen S., additional, Smith, Peter, additional, and Vincent, Jennifer L., additional

Published
2006
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39. Discovery and Optimization of a Series of Carbazole Ureas as NPY5 Antagonists for the Treatment of Obesity

Author

Block, Michael H., primary, Boyer, Scott, additional, Brailsford, Wayne, additional, Brittain, David R., additional, Carroll, Debra, additional, Chapman, Steve, additional, Clarke, David S., additional, Donald, Craig S., additional, Foote, Kevin M., additional, Godfrey, Linda, additional, Ladner, Anthony, additional, Marsham, Peter R., additional, Masters, David J., additional, Mee, Christine D., additional, O'Donovan, Michael R., additional, Pease, J. Elizabeth, additional, Pickup, Adrian G., additional, Rayner, John W., additional, Roberts, Andrew, additional, Schofield, Paul, additional, Suleman, Abid, additional, and Turnbull, Andrew V., additional

Published
2002
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40. Combined Inhibition of mTOR and BTK Signaling Is Required for Optimal Long Term Growth Inhibition in DLBCL Models

Author

Brugger, Wolfram, Hattersley, Maureen, Bussey, Alexandra, Reimer, Corinne, Tron, Adriana E., Staniszewska, Anna, Delpuech, Oona, Carnevalli, Larissa, Krejsa, Cecile M., Mayo, Michele, Neveras, Lynne, San Martin, Maryann, Rideout, Abla, Proia, Theresa, Willis, Brandon, Pease, J. Elizabeth, Hamdy, Ahmed, and Cosulich, Sabina C.

Abstract

Introduction:The mechanistic target of rapamycin (mTOR) is a serine/threonine kinase that functions as a key regulator of cell signalling, growth, metabolism and survival. Many B-cell lymphomas exhibit aberrant mTOR activation, coupled with dysregulated B-cell receptor (BCR) signalling. However, clinical trials with allosteric mTORC1 inhibitors (rapamycin and its analogues), have shown only modest efficacy in most contexts. Vistusertib (AZD2014) is an orally active dual mTORC1/2 inhibitor in clinical development for treatment of several malignancies. We investigated the potential for combining vistusertib with acalabrutinib (ACP-196), a highly selective Bruton tyrosine kinase (BTK) inhibitor, in cellular and in vivopreclinical models of diffuse large B cell lymphoma (DLBCL).

Published
2017
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41. Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-Bis anilino pyrimidines

Author

Beattie, John F., Breault, Gloria A., Ellston, Rebecca P. A., Green, Stephen, Jewsbury, Philip J., Midgley, Catherine J., Naven, Russell T., Minshull, Claire A., Pauptit, Richard A., Tucker, Julie A., and Pease, J. Elizabeth

Subjects
*CYCLIN-dependent kinases, *PYRIMIDINES, *X-ray crystallography
Abstract

Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase, CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4. [Copyright &y& Elsevier]

Published
2003
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42. Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines

Author

Breault, Gloria A., Ellston, Rebecca P. A., Green, Stephen, James, S. Russell, Jewsbury, Philip J., Midgley, Catherine J., Pauptit, Richard A., Minshull, Claire A., Tucker, Julie A., and Pease, J. Elizabeth

Subjects
*CYCLIN-dependent kinases, *PYRIMIDINES, *X-ray crystallography
Abstract

Through chemical modification and X-ray crystallography we identified the 2,4-bis anilino pyrimidines as potent inhibitors of CDK4. Herein, we describe the optimisation of this series. [Copyright &y& Elsevier]

Published
2003
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43. AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS -Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib.

Author

Flemington V, Davies EJ, Robinson D, Sandin LC, Delpuech O, Zhang P, Hanson L, Farrington P, Bell S, Falenta K, Gibbons FD, Lindsay N, Smith A, Wilson J, Roberts K, Tonge M, Hopcroft P, Willis SE, Roudier MP, Rooney C, Coker EA, Jaaks P, Garnett MJ, Fawell SE, Jones CD, Ward RA, Simpson I, Cosulich SC, Pease JE, and Smith PD

Subjects
Animals, Benzimidazoles pharmacology, Disease Models, Animal, Humans, Imidazoles pharmacology, Mice, Mice, Nude, Pyrazines pharmacology, Pyrimidines pharmacology, Benzimidazoles therapeutic use, Imidazoles therapeutic use, Proto-Oncogene Proteins p21(ras) metabolism, Pyrazines therapeutic use, Pyrimidines therapeutic use
Abstract

The RAS-regulated RAF-MEK1/2-ERK1/2 (RAS/MAPK) signaling pathway is a major driver in oncogenesis and is frequently dysregulated in human cancers, primarily by mutations in BRAF or RAS genes. The clinical benefit of inhibitors of this pathway as single agents has only been realized in BRAF -mutant melanoma, with limited effect of single-agent pathway inhibitors in KRAS -mutant tumors. Combined inhibition of multiple nodes within this pathway, such as MEK1/2 and ERK1/2, may be necessary to effectively suppress pathway signaling in KRAS -mutant tumors and achieve meaningful clinical benefit. Here, we report the discovery and characterization of AZD0364, a novel, reversible, ATP-competitive ERK1/2 inhibitor with high potency and kinase selectivity. In vitro , AZD0364 treatment resulted in inhibition of proximal and distal biomarkers and reduced proliferation in sensitive BRAF -mutant and KRAS -mutant cell lines. In multiple in vivo xenograft models, AZD0364 showed dose- and time-dependent modulation of ERK1/2-dependent signaling biomarkers resulting in tumor regression in sensitive BRAF - and KRAS -mutant xenografts. We demonstrate that AZD0364 in combination with the MEK1/2 inhibitor, selumetinib (AZD6244 and ARRY142886), enhances efficacy in KRAS -mutant preclinical models that are moderately sensitive or resistant to MEK1/2 inhibition. This combination results in deeper and more durable suppression of the RAS/MAPK signaling pathway that is not achievable with single-agent treatment. The AZD0364 and selumetinib combination also results in significant tumor regressions in multiple KRAS -mutant xenograft models. The combination of ERK1/2 and MEK1/2 inhibition thereby represents a viable clinical approach to target KRAS -mutant tumors., (©2020 American Association for Cancer Research.)

Published
2021
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44. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 L265P Diffuse Large B-Cell Lymphoma.

Author

Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, and Wu D

Subjects
Administration, Oral, Animals, Antineoplastic Agents administration & dosage, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacokinetics, Cell Line, Tumor, Crystallography, X-Ray, Dogs, Female, Humans, Interleukin-1 Receptor-Associated Kinases chemistry, Lymphoma, Large B-Cell, Diffuse genetics, Magnetic Resonance Spectroscopy, Male, Mice, SCID, Mutation, Myeloid Differentiation Factor 88 genetics, Protein Kinase Inhibitors administration & dosage, Pyrimidines chemistry, Pyrroles chemistry, Rats, Wistar, Structure-Activity Relationship, Xenograft Model Antitumor Assays, Antineoplastic Agents pharmacology, Interleukin-1 Receptor-Associated Kinases antagonists & inhibitors, Lymphoma, Large B-Cell, Diffuse drug therapy, Protein Kinase Inhibitors chemistry, Protein Kinase Inhibitors pharmacology
Abstract

Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal structures and structure based design to identify and optimize our scaffold. Compound 28 demonstrated a favorable physicochemical and kinase selectivity profile and was identified as a promising in vivo tool with which to explore the role of IRAK4 inhibition in the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma (DLBCL). Compound 28 was shown to be capable of demonstrating inhibition of NF-κB activation and growth of the ABC subtype of DLBCL cell lines in vitro at high concentrations but showed greater effects in combination with a BTK inhibitor at lower concentrations. In vivo, the combination of compound 28 and ibrutinib led to tumor regression in an ABC-DLBCL mouse model.

Published
2017
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