First-in-Man Clinical Trial of the Oral Pan-AKT Inhibitor MK-2206 in Patients With Advanced Solid Tumors
YAP, Timothy A, LI YAN, RIISNAES, Ruth, POPE, Lorna L, HEATON, Simon P, THOMAS, George, GARRETT, Michelle D, SULLIVAN, Daniel M, DE BONO, Johann S, TOLCHER, Anthony W, PATNAIK, Amita, FEAREN, Ivy, OLMOS, David, PAPADOPOULOS, Kyriakos, BAIRD, Richard D, DELGADO, Liliana, TAYLOR, Adekemi, LUPINACCI, Lisa
Published in Journal of clinical oncology (10.12.2011)
Published in Journal of clinical oncology (10.12.2011)
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AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis
WILKINSON, Robert W, ODEDRA, Rajesh, BYTH, Kate F, BARRASS, Nigel C, MUNDT, Kirsten E, FOOTE, Kevin M, HERON, Nicola M, JUNG, Frederic H, MORTLOCK, Andrew A, BOYLE, F. Thomas, GREEN, Stephen, HEATON, Simon P, WEDGE, Stephen R, KEEN, Nicholas J, CRAFTER, Claire, FOSTER, John R, BRADY, Madeleine C, BIGLEY, Alison, BROWN, Elaine
Published in Clinical cancer research (15.06.2007)
Published in Clinical cancer research (15.06.2007)
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Interrogating two schedules of the AKT inhibitor MK-2206 in patients with advanced solid tumors incorporating novel pharmacodynamic and functional imaging biomarkers
Yap, Timothy A, Yan, Li, Patnaik, Amita, Tunariu, Nina, Biondo, Andrea, Fearen, Ivy, Papadopoulos, Kyriakos P, Olmos, David, Baird, Richard, Delgado, Liliana, Tetteh, Ernestina, Beckman, Robert A, Lupinacci, Lisa, Riisnaes, Ruth, Decordova, Shaun, Heaton, Simon P, Swales, Karen, deSouza, Nandita M, Leach, Martin O, Garrett, Michelle D, Sullivan, Daniel M, de Bono, Johann S, Tolcher, Anthony W
Published in Clinical cancer research (15.11.2014)
Published in Clinical cancer research (15.11.2014)
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Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase
Mortlock, Andrew A, Foote, Kevin M, Heron, Nicola M, Jung, Frédéric H, Pasquet, Georges, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, De Savi, Chris, Roberts, Nicola J, Johnson, Trevor, Dousson, Cyril B, Hill, George B, Perkins, David, Hatter, Glenn, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Crafter, Claire, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen, Khatri, Liz, Brady, Madeleine C, Kearney, Sarah, McKillop, David, Rhead, Steve, Parry, Tony, Green, Stephen
Published in Journal of medicinal chemistry (03.05.2007)
Published in Journal of medicinal chemistry (03.05.2007)
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AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity
YAP, Timothy A, WALTON, Mike I, HEINZMANN, Kathrin, JONES, Paul S, FELTELL, Ruth E, REULE, Matthias, WOODHEAD, Steven J, DAVIES, Thomas G, LYONS, John F, RAYNAUD, Florence I, ECCLES, Suzanne A, WORKMAN, Paul, GRIMSHAW, Kyla M, THOMPSON, Neil T, GARRETT, Michelle D, TE POELE, Robert H, EVE, Paul D, VALENTI, Melanie R, DE HAVEN BRANDON, Alexis K, MARTINS, Vanessa, ZETTERLUND, Anna, HEATON, Simon P
Published in Clinical cancer research (15.07.2012)
Published in Clinical cancer research (15.07.2012)
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AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth
Grimshaw, Kyla M, Hunter, Lisa-Jane K, Yap, Timothy A, Heaton, Simon P, Walton, Mike I, Woodhead, Steven J, Fazal, Lynsey, Reule, Matthias, Davies, Thomas G, Seavers, Lisa C, Lock, Victoria, Lyons, John F, Thompson, Neil T, Workman, Paul, Garrett, Michelle D
Published in Molecular cancer therapeutics (01.05.2010)
Published in Molecular cancer therapeutics (01.05.2010)
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Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930
Yap, Timothy A, Walton, Mike I, Hunter, Lisa-Jane K, Valenti, Melanie, de Haven Brandon, Alexis, Eve, Paul D, Ruddle, Ruth, Heaton, Simon P, Henley, Alan, Pickard, Lisa, Vijayaraghavan, Gowri, Caldwell, John J, Thompson, Neil T, Aherne, Wynne, Raynaud, Florence I, Eccles, Suzanne A, Workman, Paul, Collins, Ian, Garrett, Michelle D
Published in Molecular cancer therapeutics (01.02.2011)
Published in Molecular cancer therapeutics (01.02.2011)
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Intratracheal and oral administration of SM‐276001: A selective TLR7 agonist, leads to antitumor efficacy in primary and metastatic models of cancer
Koga‐Yamakawa, Erina, Dovedi, Simon J., Murata, Masashi, Matsui, Hiroyuki, Leishman, Andrew J., Bell, John, Ferguson, Douglas, Heaton, Simon P., Oki, Toshihiro, Tomizawa, Hideyuki, Bahl, Ash, Takaku, Haruo, Wilkinson, Robert W., Harada, Hideyuki
Published in International journal of cancer (01.02.2013)
Published in International journal of cancer (01.02.2013)
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Preclinical evaluation of M30 and M65 ELISAs as biomarkers of drug induced tumor cell death and antitumor activity
Cummings, Jeffrey, Hodgkinson, Cassandra, Odedra, Rajesh, Sini, Patrizia, Heaton, Simon P, Mundt, Kirsten E, Ward, Tim H, Wilkinson, Robert W, Growcott, Jim, Hughes, Andrew, Dive, Caroline
Published in Molecular cancer therapeutics (01.03.2008)
Published in Molecular cancer therapeutics (01.03.2008)
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Novel pharmacodynamic biomarkers for MYCN protein and PI3K/AKT/mTOR pathway signaling in children with neuroblastoma
Smith, Jennifer R., Moreno, Lucas, Heaton, Simon P., Chesler, Louis, Pearson, Andrew D.J., Garrett, Michelle D.
Published in Molecular oncology (01.04.2016)
Published in Molecular oncology (01.04.2016)
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Journal Article
Discovery of Novel and Potent Thiazoloquinazolines as Selective Aurora A and B Kinase Inhibitors
Jung, Frédéric H, Pasquet, Georges, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, Germain, Hervé, De Savi, Chris, Roberts, Nicola, Johnson, Trevor, Dousson, Cyril, Hill, George B, Mortlock, Andrew A, Heron, Nicola, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Green, Stephen, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen
Published in Journal of medicinal chemistry (09.02.2006)
Published in Journal of medicinal chemistry (09.02.2006)
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Journal Article
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: Selective inhibitors of Aurora B kinase with potent anti-tumor activity
Foote, Kevin M., Mortlock, Andrew A., Heron, Nicola M., Jung, Frédéric H., Hill, George B., Pasquet, Georges, Brady, Madeleine C., Green, Stephen, Heaton, Simon P., Kearney, Sarah, Keen, Nicholas J., Odedra, Rajesh, Wedge, Stephen R., Wilkinson, Robert W.
Published in Bioorganic & medicinal chemistry (15.03.2008)
Published in Bioorganic & medicinal chemistry (15.03.2008)
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Miscellaneous: P22: The value of automated cellular imaging on tissue microarrays in the drug-discovery process
Bigley, Alison L., Brocklehurst, Simon R., Randall, Kevin J., Jenkins, Richard P., Wilkinson, Robert W., Heaton, Simon P., Foster, John, Hughes, Gareth D., McKay, Jennifer S.
Published in Experimental and toxicologic pathology : official journal of the Gesellschaft für Toxikologische Pathologie (01.05.2009)
Published in Experimental and toxicologic pathology : official journal of the Gesellschaft für Toxikologische Pathologie (01.05.2009)
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Abstract 931: The combination of the dual mTORC1/mTORC2 inhibitor AZD2014 and paclitaxel in human ovarian cancer models
Stewart, Adam, Thavasu, Parames, Heaton, Simon, Banerjee, Susana, Kaye, Stan B., Banerji, Udai
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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Abstract 4434: Combined targeting of Aurora B (AZD1152) and MEK1/2 (AZD6244) kinases leads to enhancement of anti-tumour effects in vivo
Odedra, Rajesh, Heaton, Simon, Logie, Armelle, Mundt, Kirsten E., Anderson, Elizabeth, Smith, Paul D., Wilkinson, Robert W.
Published in Cancer research (Chicago, Ill.) (15.04.2010)
Published in Cancer research (Chicago, Ill.) (15.04.2010)
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A pharmacokinetic (PK) pharmacodynamic (PD) driven first-in-human study of the oral class I PI3K inhibitor CH5132799, in patients with advanced solid tumors
Omlin, Aurelius Gabriel, Spicer, James F., Sarker, Debashis, Pinato, David James, Agarwal, Roshan, Cassier, Philippe Alexandre, Stavraka, Chara, Blanco, Monsterrat, Suder, Aneta, Allan, Suzanne, Heaton, Simon, Decordova, Shaun, Pope, Lorna, Prince, Jenny, Noguchi, Kohei, Jones, Keith, Inatani, Michiyasu, Shiokawa, Rie, Banerji, Udai, Blagden, Sarah Patricia
Published in Journal of clinical oncology (20.05.2012)
Published in Journal of clinical oncology (20.05.2012)
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Abstract 928: The novel clinical candidate AT13148 is an oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity and demonstrates a mechanism of action distinct from AKT inhibitors
Yap, Timothy A., Walton, Michael I., Grimshaw, Kyla M., Poele, Robert H. te, Eve, Paul D., Valenti, Melanie R., de Haven Brandon, Alexis K., Martins, Vanessa, Zetterlund, Anna, Heaton, Simon P., Heinzmann, Kathrin, Jones, Paul S., Feltell, Ruth E., Reule, Matthias, Woodhead, Steven J., Davies, Thomas G., Lyons, John F., Raynaud, Florence I., Eccles, Suzanne A., Workman, Paul, Thompson, Neil T., Garrett, Michelle D.
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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Abstract 5440: Study of the mechanism of action and pharmacodynamic response of JNJ-26481585, a potent histone deacetylase inhibitor in the setting of melanoma
Poele, Robert Te, Heaton, Simon, Garrett, Michelle, Hellemans, Peter, Hickson, Ian, Sand-Dejmek, Janna, Evans, Jeffrey TR, de Bono, Johann S., Banerji, Udai
Published in Cancer research (Chicago, Ill.) (15.04.2010)
Published in Cancer research (Chicago, Ill.) (15.04.2010)
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Abstract 4481: First report of preclinical pharmacology of two novel potent AKT inhibitors and development of pharmacodynamic (PD) biomarkers in tumor and surrogate tissue
Yap, Timothy A., Walton, Mike I., Hunter, Lisa, Grimshaw, Kyla, Valenti, Melanie, Eve, Paul, Heaton, Simon P., Pickard, Lisa, Caldwell, John J., Thompson, Neil, de Bono, Johann S., Kaye, Stan B., Eccles, Sue A., Workman, Paul, Collins, Ian, Garrett, Michelle D.
Published in Cancer research (Chicago, Ill.) (15.04.2010)
Published in Cancer research (Chicago, Ill.) (15.04.2010)
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