Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014 von Pike, Kurt G., Malagu, Karine, Hummersone, Marc G., Menear, Keith A., Duggan, Heather M.E., Gomez, Sylvie, Martin, Niall M.B., Ruston, Linette, Pass, Sarah L., Pass, Martin

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Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion von Golding, Sarah E, Rosenberg, Elizabeth, Valerie, Nicholas, Hussaini, Isa, Frigerio, Mark, Cockcroft, Xiaoling F, Chong, Wei Yee, Hummersone, Marc, Rigoreau, Laurent, Menear, Keith A, O'Connor, Mark J, Povirk, Lawrence F, van Meter, Timothy, Valerie, Kristoffer

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4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1 von Menear, Keith A, Adcock, Claire, Boulter, Robert, Cockcroft, Xiao-ling, Copsey, Louise, Cranston, Aaron, Dillon, Krystyna J, Drzewiecki, Jan, Garman, Sheila, Gomez, Sylvie, Javaid, Hashim, Kerrigan, Frank, Knights, Charlotte, Lau, Alan, Loh, Vincent M, Matthews, Ian T. W, Moore, Stephen, O’Connor, Mark J, Smith, Graeme C. M, Martin, Niall M. B

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Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K von Munck, Joanne M, Batey, Michael A, Zhao, Yan, Jenkins, Helen, Richardson, Caroline J, Cano, Celine, Tavecchio, Michele, Barbeau, Jody, Bardos, Julia, Cornell, Liam, Griffin, Roger J, Menear, Keith, Slade, Andrew, Thommes, Pia, Martin, Niall M B, Newell, David R, Smith, Graeme C M, Curtin, Nicola J

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1‑Substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino‑4H‑chromen-4-ones Endowed with Dual DNA-PK/PI3‑K Inhibitory Activity von Cano, Céline, Saravanan, Kappusamy, Bailey, Chris, Bardos, Julia, Curtin, Nicola J, Frigerio, Mark, Golding, Bernard T, Hardcastle, Ian R, Hummersone, Marc G, Menear, Keith A, Newell, David R, Richardson, Caroline J, Shea, K, Smith, Graeme C. M, Thommes, Pia, Ting, Attilla, Griffin, Roger J

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DNA-Dependent Protein Kinase (DNA-PK) Inhibitors. Synthesis and Biological Activity of Quinolin-4-one and Pyridopyrimidin-4-one Surrogates for the Chromen-4-one Chemotype von Cano, Céline, Barbeau, Olivier R, Bailey, Christine, Cockcroft, Xiao-Ling, Curtin, Nicola J, Duggan, Heather, Frigerio, Mark, Golding, Bernard T, Hardcastle, Ian R, Hummersone, Marc G, Knights, Charlotte, Menear, Keith A, Newell, David R, Richardson, Caroline J, Smith, Graeme C. M, Spittle, Ben, Griffin, Roger J

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Pyranone, Thiopyranone, and Pyridone Inhibitors of Phosphatidylinositol 3-Kinase Related Kinases. Structure−Activity Relationships for DNA-Dependent Protein Kinase Inhibition, and... von Hollick, Jonathan J, Rigoreau, Laurent J. M, Cano-Soumillac, Celine, Cockcroft, Xiaoling, Curtin, Nicola J, Frigerio, Mark, Golding, Bernard T, Guiard, Sophie, Hardcastle, Ian R, Hickson, Ian, Hummersone, Marc G, Menear, Keith A, Martin, Niall M. B, Matthews, Ian, Newell, David R, Ord, Rachel, Richardson, Caroline J, Smith, Graeme C. M, Griffin, Roger J

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Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR von Menear, Keith A., Gomez, Sylvie, Malagu, Karine, Bailey, Christine, Blackburn, Kristel, Cockcroft, Xiao-Ling, Ewen, Sally, Fundo, Alexandra, Gall, Armelle Le, Hermann, Gesine, Sebastian, Luisa, Sunose, Mihiro, Presnot, Thomas, Torode, Eleanor, Hickson, Ian, Martin, Niall M.B., Smith, Graeme C.M., Pike, Kurt G.

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DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain von Clapham, Kate M., Bardos, Julia, Finlay, M. Raymond V., Golding, Bernard T., Griffen, Edward J., Griffin, Roger J., Hardcastle, Ian R., Menear, Keith A., Ting, Attilla, Turner, Paul, Young, Gail L., Cano, Céline

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Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase von Loh, Vincent M., Cockcroft, Xiao-ling, Dillon, Krystyna J., Dixon, Lesley, Drzewiecki, Jan, Eversley, Penny J., Gomez, Sylvie, Hoare, Janet, Kerrigan, Frank, Matthews, Ian T.W., Menear, Keith A., Martin, Niall M.B., Newton, Roger F., Paul, Jane, Smith, Graeme C.M., Vile, Julia, Whittle, Alan J.

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Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase von Cockcroft, Xiao-ling, Dillon, Krystyna J., Dixon, Lesley, Drzewiecki, Jan, Kerrigan, Frank, Loh, Vincent M., Martin, Niall M.B., Menear, Keith A., Smith, Graeme C.M.

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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase von Menear, Keith A., Adcock, Claire, Alonso, Francisco Cuenca, Blackburn, Kristel, Copsey, Louise, Drzewiecki, Jan, Fundo, Alexandra, Le Gall, Armelle, Gomez, Sylvie, Javaid, Hashim, Lence, Carlos Fenandez, Martin, Niall M.B., Mydlowski, Chris, Smith, Graeme C.M.

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AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity von CHRESTA, Christine M, DAVIES, Barry R, JAMES, Dominic, HOWARD, Zoe, DUDLEY, Phillippa, HUGHES, Gareth, SMITH, Lisa, MAGUIRE, Sharon, HUMMERSONE, Marc, MALAGU, Karine, MENEAR, Keith, JENKINS, Richard, HICKSON, Ian, JACOBSEN, Matt, SMITH, Graeme C. M, GUICHARD, Sylvie, PASS, Martin, HARDING, Tom, COSULICH, Sabina, CRITCHLOW, Susan E, VINCENT, John P, ELLSTON, Rebecca, JONES, Darren, SINI, Patrizia

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Abstract A110: Hypoxia-selective DNA-PK inhibitor von Kyle, Alastair H., Baker, Jennifer H.E., Fryer, Karen H., Banaáth, Judit, Wang, Taixiang, Porres, Soraya S., Mann, Sam E., Hynd, George, Menear, Keith, Minchinton, Andrew I.

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1-Substituted (Dibenzo[ b,d ]thiophen-4-yl)-2-morpholino-4 H -chromen-4-ones Endowed with Dual DNA-PK/PI3-K Inhibitory Activity von Cano, Céline, Saravanan, Kappusamy, Bailey, Chris, Bardos, Julia, Curtin, Nicola J., Frigerio, Mark, Golding, Bernard T., Hardcastle, Ian R., Hummersone, Marc G., Menear, Keith A., Newell, David R., Richardson, Caroline J., Shea, K., Smith, Graeme C. M., Thommes, Pia, Ting, Attilla, Griffin, Roger J.

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The discovery and optimisation of pyrido[2,3- d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase von Malagu, Karine, Duggan, Heather, Menear, Keith, Hummersone, Marc, Gomez, Sylvie, Bailey, Christine, Edwards, Peter, Drzewiecki, Jan, Leroux, Frédéric, Quesada, Mar Jimenez, Hermann, Gesine, Maine, Stephanie, Molyneaux, Carrie-Anne, Le Gall, Armelle, Pullen, James, Hickson, Ian, Smith, Lisa, Maguire, Sharon, Martin, Niall, Smith, Graeme, Pass, Martin

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The P 1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin von Yamaguchi, Yasuchika, Menear, Keith, Cohen, Nissim-Claude, Mah, Robert, Cumin, Frédéric, Schnell, Christian, Wood, Jeanette M., Maibaum, Jürgen

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The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin von YAMAGUCHI, Yasuchika, MENEAR, Keith, COHEN, Nissim-Claude, MAH, Robert, CUMIN, Frédéric, SCHNELL, Christian, WOOD, Jeanette M, MAIBAUM, Jürgen

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Direct thrombin inhibitors: current status and future prospects von Menear, Keith

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Abstract A116: Radio- and chemosensitization through inhibition of DNA-PK by KU-0060648 von Bardos, Julia, Shea, Kerry, Parveen, Nahida, Peacock, Marcus, Deacon, William, Cranston, Aaron, Albertella, Mark, Menear, Keith, Smith, Graeme, Martin, Niall

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