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2. Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390

Author

Pike, Kurt G., primary, Hunt, Thomas A., additional, Barlaam, Bernard, additional, Benstead, David, additional, Cadogan, Elaine, additional, Chen, Kan, additional, Cook, Calum R., additional, Colclough, Nicola, additional, Deng, Chao, additional, Durant, Stephen T., additional, Eatherton, Andrew, additional, Goldberg, Kristin, additional, Johnström, Peter, additional, Liu, Libin, additional, Liu, Zhaoqun, additional, Nissink, J. Willem M., additional, Pang, Chengling, additional, Pass, Martin, additional, Robb, Graeme R., additional, Roberts, Caroline, additional, Schou, Magnus, additional, Steward, Oliver, additional, Sykes, Andy, additional, Yan, Yumei, additional, Zhai, Baochang, additional, and Zheng, Li, additional

Published
2024
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4. Video 1 - ATMi increases the rate of mitotic catastrophe in glioma cells when p53 is knocked down. from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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5. Video 4 - ATMi increases the rate of mitotic catastrophe in glioma cells when p53 is knocked down. from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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6. Data from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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7. Supplemenary Figure 2 from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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8. Supplementary Tables 1 through 4 from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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9. Supplementary figure 1 from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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10. Data from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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11. Supplementary methods from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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12. Supplementary Information from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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13. Video 2 - ATMi increases the rate of mitotic catastrophe in glioma cells when p53 is knocked down. from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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14. Video 3 - ATMi increases the rate of mitotic catastrophe in glioma cells when p53 is knocked down. from Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, primary, Ahmad, Syed F., primary, Hughes, Gareth, primary, Sheridan, Victoria, primary, Odedra, Rajesh, primary, Farrington, Paul, primary, Cadogan, Elaine B., primary, Riches, Lucy C., primary, Garcia-Trinidad, Antonio, primary, Thomason, Andrew G., primary, Patel, Bhavika, primary, Vincent, Jennifer, primary, Lau, Alan, primary, Pike, Kurt G., primary, Hunt, Thomas A., primary, Sule, Amrita, primary, Valerie, Nicholas C.K., primary, Biddlestone-Thorpe, Laura, primary, Kahn, Jenna, primary, Beckta, Jason M., primary, Mukhopadhyay, Nitai, primary, Barlaam, Bernard, primary, Degorce, Sebastien L., primary, Kettle, Jason, primary, Colclough, Nicola, primary, Wilson, Joanne, primary, Smith, Aaron, primary, Barrett, Ian P., primary, Zheng, Li, primary, Zhang, Tianwei, primary, Wang, Yingchun, primary, Chen, Kan, primary, Pass, Martin, primary, Durant, Stephen T., primary, and Valerie, Kristoffer, primary

Published
2023
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15. Supplementary figure 4 from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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16. Supplementary figure 3 from AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, primary, Bihani, Teeru, primary, D'Cruz, Celina M., primary, Yates, James W.T., primary, Grondine, Michael, primary, Howard, Zoe, primary, Davies, Barry R., primary, Bigley, Graham, primary, Klinowska, Teresa, primary, Pike, Kurt G., primary, Pass, Martin, primary, Chresta, Christine M., primary, Polanska, Urszula M., primary, McEwen, Robert, primary, Delpuech, Oona, primary, Green, Stephen, primary, and Cosulich, Sabina C., primary

Published
2023
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17. Inhibitors of the Fibroblast Growth Factor Receptor

Author

Pike, Kurt G., Bernstein, P. R., Editorial Board Member, Buschauer, A. L., Editorial Board Member, Georg, G. I., Editorial Board Member, Kobayashi, T., Editorial Board Member, Lowe, J. A., Editorial Board Member, Meanwell, N. A., Editorial Board Member, Saxena, A. K., Editorial Board Member, Stilz, U., Editorial Board Member, Supuran, C. T., Editorial Board Member, Zhang, A., Editorial Board Member, Waring, Michael J., editor, Campbell, J. E., Book Editor, Cano, C., Book Editor, Duncan, K. W., Book Editor, Finlay, M. R. V., Book Editor, Gray, N. S., Book Editor, Hardcastle, I. R., Book Editor, Harnor, S., Book Editor, Harris, P. A., Book Editor, Hatcher, J. M., Book Editor, Manley, P. W., Book Editor, Michielin, O., Book Editor, Pan, Z., Book Editor, Pickles, J., Book Editor, Pike, K. G., Book Editor, Röhrig, U. F., Book Editor, Staben, S. T., Book Editor, Stiefl, N. J., Book Editor, Toader, D., Book Editor, Ward, R. A., Book Editor, Zoete, V., Book Editor, and Zuo, Y., Book Editor

Published
2018
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19. Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase

Author

Bagal, Sharan K., primary, Gregson, Clare, additional, O’ Donovan, Daniel H., additional, Pike, Kurt G., additional, Bloecher, Andrew, additional, Barton, Peter, additional, Borodovsky, Alexandra, additional, Code, Erin, additional, Fillery, Shaun M., additional, Hsu, Jessie Hao-Ru, additional, Kawatkar, Sameer P., additional, Li, Chengzhi, additional, Longmire, David, additional, Nai, Youfeng, additional, Nash, Samuel C., additional, Pike, Andrew, additional, Robinson, James, additional, Read, Jon A., additional, Rawlins, Phillip B., additional, Shen, Minhui, additional, Tang, Jia, additional, Wang, Peng, additional, Woods, Haley, additional, and Williamson, Beth, additional

Published
2021
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20. Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement

Author

Barlaam, Bernard, primary, De Savi, Chris, additional, Dishington, Allan, additional, Drew, Lisa, additional, Ferguson, Andrew D., additional, Ferguson, Douglas, additional, Gu, Chungang, additional, Hande, Sudhir, additional, Hassall, Lorraine, additional, Hawkins, Janet, additional, Hird, Alexander W., additional, Holmes, Jane, additional, Lamb, Michelle L., additional, Lister, Andrew S., additional, McGuire, Thomas M., additional, Moore, Jane E., additional, O’Connell, Nichole, additional, Patel, Anil, additional, Pike, Kurt G., additional, Sarkar, Ujjal, additional, Shao, Wenlin, additional, Stead, Darren, additional, Varnes, Jeffrey G., additional, Vasbinder, Melissa M., additional, Wang, Lei, additional, Wu, Liangwei, additional, Xue, Lin, additional, Yang, Bin, additional, and Yao, Tieguang, additional

Published
2021
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22. Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

Author

Barlaam, Bernard, primary, Casella, Robert, additional, Cidado, Justin, additional, Cook, Calum, additional, De Savi, Chris, additional, Dishington, Allan, additional, Donald, Craig S., additional, Drew, Lisa, additional, Ferguson, Andrew D., additional, Ferguson, Douglas, additional, Glossop, Steve, additional, Grebe, Tyler, additional, Gu, Chungang, additional, Hande, Sudhir, additional, Hawkins, Janet, additional, Hird, Alexander W., additional, Holmes, Jane, additional, Horstick, James, additional, Jiang, Yun, additional, Lamb, Michelle L., additional, McGuire, Thomas M., additional, Moore, Jane E., additional, O’Connell, Nichole, additional, Pike, Andy, additional, Pike, Kurt G., additional, Proia, Theresa, additional, Roberts, Bryan, additional, San Martin, Maryann, additional, Sarkar, Ujjal, additional, Shao, Wenlin, additional, Stead, Darren, additional, Sumner, Neil, additional, Thakur, Kumar, additional, Vasbinder, Melissa M., additional, Varnes, Jeffrey G., additional, Wang, Jianyan, additional, Wang, Lei, additional, Wu, Dedong, additional, Wu, Liangwei, additional, Yang, Bin, additional, and Yao, Tieguang, additional

Published
2020
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23. Pharmacology of the ATM Inhibitor AZD0156: Potentiation of Irradiation and Olaparib Responses Preclinically

Author

Riches, Lucy C., primary, Trinidad, Antonio G., additional, Hughes, Gareth, additional, Jones, Gemma N., additional, Hughes, Adina M., additional, Thomason, Andrew G., additional, Gavine, Paul, additional, Cui, Andy, additional, Ling, Stephanie, additional, Stott, Jonathan, additional, Clark, Roger, additional, Peel, Samantha, additional, Gill, Pendeep, additional, Goodwin, Louise M., additional, Smith, Aaron, additional, Pike, Kurt G., additional, Barlaam, Bernard, additional, Pass, Martin, additional, O'Connor, Mark J., additional, Smith, Graeme, additional, and Cadogan, Elaine B., additional

Published
2020
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24. General methods for the synthesis and late-stage diversification of 2,4-substituted 7-azaindoles

Author

Varnes, Jeffrey G., McGuire, Thomas, Meadows, Rebecca E., Barlaam, Bernard, Clark, Jemma, Cook, Calum R., Davison, Gemma, Dishington, Allan, De Savi, Chris, Donald, Craig, Grebe, Tyler, Hande, Sudhir, Hawkins, Janet, Hird, Alexander W., Holmes, Jane, Lister, Andrew, Lucas, Simon, Moore, Jane, Moore, Esther, Patel, Anil, Pike, Kurt G., Roberts, Bryan, Stark, Andrew, Stead, Darren, Thakur, Kumar, Turner, Paul, Vasbinder, Melissa, and Yang, Bin

Published
2016
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25. Orally Bioavailable and Blood–Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

Author

Karlin, Jeremy, primary, Allen, Jasmine, additional, Ahmad, Syed F., additional, Hughes, Gareth, additional, Sheridan, Victoria, additional, Odedra, Rajesh, additional, Farrington, Paul, additional, Cadogan, Elaine B., additional, Riches, Lucy C., additional, Garcia-Trinidad, Antonio, additional, Thomason, Andrew G., additional, Patel, Bhavika, additional, Vincent, Jennifer, additional, Lau, Alan, additional, Pike, Kurt G., additional, Hunt, Thomas A., additional, Sule, Amrita, additional, Valerie, Nicholas C.K., additional, Biddlestone-Thorpe, Laura, additional, Kahn, Jenna, additional, Beckta, Jason M., additional, Mukhopadhyay, Nitai, additional, Barlaam, Bernard, additional, Degorce, Sebastien L., additional, Kettle, Jason, additional, Colclough, Nicola, additional, Wilson, Joanne, additional, Smith, Aaron, additional, Barrett, Ian P., additional, Zheng, Li, additional, Zhang, Tianwei, additional, Wang, Yingchun, additional, Chen, Kan, additional, Pass, Martin, additional, Durant, Stephen T., additional, and Valerie, Kristoffer, additional

Published
2018
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26. Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors

Author

Barlaam, Bernard, primary, Cadogan, Elaine, additional, Campbell, Andrew, additional, Colclough, Nicola, additional, Dishington, Allan, additional, Durant, Stephen, additional, Goldberg, Kristin, additional, Hassall, Lorraine A., additional, Hughes, Gareth D., additional, MacFaul, Philip A., additional, McGuire, Thomas M., additional, Pass, Martin, additional, Patel, Anil, additional, Pearson, Stuart, additional, Petersen, Jens, additional, Pike, Kurt G., additional, Robb, Graeme, additional, Stratton, Natalie, additional, Xin, Guohong, additional, and Zhai, Baochang, additional

Published
2018
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27. Correction to Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Author

Degorce, Sébastien L., primary, Barlaam, Bernard, additional, Cadogan, Elaine, additional, Dishington, Allan, additional, Ducray, Richard, additional, Glossop, Steven C., additional, Hassall, Lorraine A., additional, Lach, Franck, additional, Lau, Alan, additional, McGuire, Thomas M., additional, Nowak, Thorsten, additional, Ouvry, Gilles, additional, Pike, Kurt G., additional, and Thomason, Andrew G., additional

Published
2018
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28. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models

Author

Durant, Stephen T., primary, Zheng, Li, additional, Wang, Yingchun, additional, Chen, Kan, additional, Zhang, Lingli, additional, Zhang, Tianwei, additional, Yang, Zhenfan, additional, Riches, Lucy, additional, Trinidad, Antonio G., additional, Fok, Jacqueline H. L., additional, Hunt, Tom, additional, Pike, Kurt G., additional, Wilson, Joanne, additional, Smith, Aaron, additional, Colclough, Nicola, additional, Reddy, Venkatesh Pilla, additional, Sykes, Andrew, additional, Janefeldt, Annika, additional, Johnström, Peter, additional, Varnäs, Katarina, additional, Takano, Akihiro, additional, Ling, Stephanie, additional, Orme, Jonathan, additional, Stott, Jonathan, additional, Roberts, Caroline, additional, Barrett, Ian, additional, Jones, Gemma, additional, Roudier, Martine, additional, Pierce, Andrew, additional, Allen, Jasmine, additional, Kahn, Jenna, additional, Sule, Amrita, additional, Karlin, Jeremy, additional, Cronin, Anna, additional, Chapman, Melissa, additional, Valerie, Kristoffer, additional, Illingworth, Ruth, additional, and Pass, Martin, additional

Published
2018
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29. The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one)

Author

Pike, Kurt G., primary, Barlaam, Bernard, additional, Cadogan, Elaine, additional, Campbell, Andrew, additional, Chen, Yingxue, additional, Colclough, Nicola, additional, Davies, Nichola L., additional, de-Almeida, Camila, additional, Degorce, Sebastien L., additional, Didelot, Myriam, additional, Dishington, Allan, additional, Ducray, Richard, additional, Durant, Stephen T., additional, Hassall, Lorraine A., additional, Holmes, Jane, additional, Hughes, Gareth D., additional, MacFaul, Philip A., additional, Mulholland, Keith R., additional, McGuire, Thomas M., additional, Ouvry, Gilles, additional, Pass, Martin, additional, Robb, Graeme, additional, Stratton, Natalie, additional, Wang, Zhenhua, additional, Wilson, Joanne, additional, Zhai, Baochang, additional, Zhao, Kang, additional, and Al-Huniti, Nidal, additional

Published
2018
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30. Abstract A104: AZD1390, a potent and selective orally bioavailable blood-brain barrier-penetrant ATM inhibitor, radiosensitizes and improves survival of orthotopic glioma and metastatic brain tumor models

Author

Durant, Steve T., primary, Pike, Kurt G., additional, Colclough, Nicola, additional, Riches, Lucy, additional, Garcia-Trinidad, Antonio, additional, Hunt, Thomas, additional, Ling, Stephanie, additional, Stott, Jonathan, additional, Barrett, Ian, additional, Zheng, Li, additional, Wang, Yingchun, additional, Chen, Kan, additional, Zhang, Tianwei, additional, Pilla Reddy, Venkatesh, additional, Sykes, Andrew, additional, Johnstrom, Peter, additional, Jones, Gemma, additional, Pierce, Andrew, additional, Karlin, Jeremy, additional, Kahn, Jenna, additional, Allen, Jasmine, additional, Valerie, Kristoffer, additional, Illingworth, Ruth, additional, and Pass, Martin, additional

Published
2018
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32. Targeting the kinase activities of ATR and ATM exhibits therapeutic potential in a mouse model of MLL-rearranged AML

Author

Morgado-Palacin, Isabel, Day, Amanda, Murga, Matilde, Lafarga, Vanesa, Anton, Marta Elena, Tubbs, Anthony, Chen, Hua Tang, Ergan, Aysegul, Anderson, Rhonda, Bhandoola, Avinash, Pike, Kurt G., Barlaam, Bernard, Cadogan, Elaine, Wang, Xi, Pierce, Andrew J., Hubbard, Chad, Armstrong, Scott A., Nussenzweig, André, and Fernandez-Capetillo, Oscar

Subjects
Gene Rearrangement, Leukemia, Myeloid, Acute, Mice, hemic and lymphatic diseases, Animals, Humans, Ataxia Telangiectasia Mutated Proteins, Histone-Lysine N-Methyltransferase, Neoplasms, Experimental, neoplasms, Xenograft Model Antitumor Assays, Article, Myeloid-Lymphoid Leukemia Protein
Abstract

Among the various subtypes of acute myeloid leukemia (AML), those with chromosomal rearrangements of the MLL oncogene (AML-MLL) have a poor prognosis. AML-MLL tumor cells are resistant to current genotoxic therapies because of an attenuated response by p53, a protein that induces cell cycle arrest and apoptosis in response to DNA damage. In addition to chemicals that damage DNA, efforts have focused on targeting DNA repair enzymes as a general chemotherapeutic approach to cancer treatment. Here, we found that inhibition of the kinase ATR, which is the primary sensor of DNA replication stress, induced chromosomal breakage and death of mouse AML(MLL) cells (with an MLL-ENL fusion and a constitutively active N-RAS independently of p53. Moreover, ATR inhibition as a single agent exhibited antitumoral activity, both reducing tumor burden after establishment and preventing tumors from growing, in an immunocompetent allograft mouse model of AML(MLL) and in xenografts of a human AML-MLL cell line. We also found that inhibition of ATM, a kinase that senses DNA double-strand breaks, also promoted the survival of the AML(MLL) mice. Collectively, these data indicated that ATR or ATM inhibition represent potential therapeutic strategies for the treatment of AML, especially MLL-driven leukemias.

Published
2016

35. Targeting the kinase activities of ATR and ATM exhibits antitumoral activity in mouse models of MLL -rearranged AML

Author

Morgado-Palacin, Isabel, primary, Day, Amanda, additional, Murga, Matilde, additional, Lafarga, Vanesa, additional, Anton, Marta Elena, additional, Tubbs, Anthony, additional, Chen, Hua-Tang, additional, Ergen, Aysegul V., additional, Anderson, Rhonda, additional, Bhandoola, Avinash, additional, Pike, Kurt G., additional, Barlaam, Bernard, additional, Cadogan, Elaine, additional, Wang, Xi, additional, Pierce, Andrew J., additional, Hubbard, Chad, additional, Armstrong, Scott A., additional, Nussenzweig, André, additional, and Fernandez-Capetillo, Oscar, additional

Published
2016
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37. Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase

Author

Degorce, Sébastien L., primary, Barlaam, Bernard, additional, Cadogan, Elaine, additional, Dishington, Allan, additional, Ducray, Richard, additional, Glossop, Steven C., additional, Hassall, Lorraine A., additional, Lach, Franck, additional, Lau, Alan, additional, McGuire, Thomas M., additional, Nowak, Thorsten, additional, Ouvry, Gilles, additional, Pike, Kurt G., additional, and Thomason, Andrew G., additional

Published
2016
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38. Correction: Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9. See DOI: 10.1039/c6md00159a

Author

Rye, Carl S., primary, Chessum, Nicola E. A., additional, Lamont, Scott, additional, Pike, Kurt G., additional, Faulder, Paul, additional, Demeritt, Julie, additional, Kemmitt, Paul, additional, Tucker, Julie, additional, Zani, Lorenzo, additional, Cheeseman, Matthew D., additional, Isaac, Rosie, additional, Goodwin, Louise, additional, Boros, Joanna, additional, Raynaud, Florence, additional, Hayes, Angela, additional, Henley, Alan T., additional, de Billy, Emmanuel, additional, Lynch, Christopher J., additional, Sharp, Swee Y., additional, te Poele, Robert, additional, Fee, Lisa O’, additional, Foote, Kevin M., additional, Green, Stephen, additional, Workman, Paul, additional, and Jones, Keith, additional

Published
2016
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39. Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9

Author

Rye, Carl S., primary, Chessum, Nicola E. A., additional, Lamont, Scott, additional, Pike, Kurt G., additional, Faulder, Paul, additional, Demeritt, Julie, additional, Kemmitt, Paul, additional, Tucker, Julie, additional, Zani, Lorenzo, additional, Cheeseman, Matthew D., additional, Isaac, Rosie, additional, Goodwin, Louise, additional, Boros, Joanna, additional, Raynaud, Florence, additional, Hayes, Angela, additional, Henley, Alan T., additional, de Billy, Emmanuel, additional, Lynch, Christopher J., additional, Sharp, Swee Y., additional, te Poele, Robert, additional, Fee, Lisa O’, additional, Foote, Kevin M., additional, Green, Stephen, additional, Workman, Paul, additional, and Jones, Keith, additional

Published
2016
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42. AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Author

Guichard, Sylvie M., primary, Curwen, Jon, additional, Bihani, Teeru, additional, D'Cruz, Celina M., additional, Yates, James W.T., additional, Grondine, Michael, additional, Howard, Zoe, additional, Davies, Barry R., additional, Bigley, Graham, additional, Klinowska, Teresa, additional, Pike, Kurt G., additional, Pass, Martin, additional, Chresta, Christine M., additional, Polanska, Urszula M., additional, McEwen, Robert, additional, Delpuech, Oona, additional, Green, Stephen, additional, and Cosulich, Sabina C., additional

Published
2015
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43. Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2

Author

Pike, Kurt G., primary, Morris, Jeff, additional, Ruston, Linette, additional, Pass, Sarah L., additional, Greenwood, Ryan, additional, Williams, Emma J., additional, Demeritt, Julie, additional, Culshaw, Janet D., additional, Gill, Kristy, additional, Pass, Martin, additional, Finlay, M. Raymond V., additional, Good, Catherine J., additional, Roberts, Craig A., additional, Currie, Gordon S., additional, Blades, Kevin, additional, Eden, Jonathan M., additional, and Pearson, Stuart E., additional

Published
2015
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44. Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology

Author

Johannes, Jeffrey W., primary, Almeida, Lynsie, additional, Barlaam, Bernard, additional, Boriack-Sjodin, P. Ann, additional, Casella, Robert, additional, Croft, Rosemary A., additional, Dishington, Allan P., additional, Gingipalli, Lakshmaiah, additional, Gu, Chungang, additional, Hawkins, Janet L., additional, Holmes, Jane L., additional, Howard, Tina, additional, Huang, Jian, additional, Ioannidis, Stephanos, additional, Kazmirski, Steven, additional, Lamb, Michelle L., additional, McGuire, Thomas M., additional, Moore, Jane E., additional, Ogg, Derek, additional, Patel, Anil, additional, Pike, Kurt G., additional, Pontz, Timothy, additional, Robb, Graeme R., additional, Su, Nancy, additional, Wang, Haiyun, additional, Wu, Xiaoyun, additional, Zhang, Hai-Jun, additional, Zhang, Yue, additional, Zheng, Xiaolan, additional, and Wang, Tao, additional

Published
2015
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48. Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles.

Author

Holmes, Jane L., Almeida, Lynsie, Barlaam, Bernard, Croft, Rosemary A., Dishington, Allan P., Gingipalli, Laksmaiah, Hassall, Lorraine A., Hawkins, Janet L., Ioannidis, Stephanos, Johannes, Jeffrey W., McGuire, Thomas M., Moore, Jane E., Patel, Anil, Pike, Kurt G., Pontz, Timothy, Xiaoyun Wu, Tao Wang, Hai-Jun Zhang, and Xiaolan Zheng

Subjects
CHEMICAL synthesis, HYDROXYMETHYL compounds, HETEROCYCLIC compounds, ISOQUINOLINE, PQQ (Biochemistry)
Abstract

Examples of hydroxymethylated analogues of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4- d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin- 4(3H)-ones are sparse or non-existent in the scientific literature. We have demonstrated that such compounds are accessible by using standard procedures from readily available raw materials. [ABSTRACT FROM AUTHOR]

Published
2016
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