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Neil T. Thompson
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Journal Articles

ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK

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Joanne M. Munck, Valerio Berdini, Luke Bevan, Jessica L. Brothwood, Juan Castro, Aurélie Courtin, Charlotte East, Roberta Ferraldeschi, Tom D. Heightman, Christopher J. Hindley, Justyna Kucia-Tran, John F. Lyons, Vanessa Martins, Sandra Muench, Christopher W. Murray, David Norton, Marc O'Reilly, Michael Reader, David C. Rees, Sharna J. Rich, Caroline J. Richardson, Alpesh D. Shah, Lukas Stanczuk, Neil T. Thompson, Nicola E. Wilsher, Alison J.-A. Woolford, Nicola G. Wallis
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2021) 20 (10): 1757–1768.
https://doi.org/10.1158/1535-7163.MCT-20-0909
Published: 01 October 2021
View articletitled, ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK
Open the PDF for ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK in another window
Includes: Supplementary data
Journal Articles

ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth

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George A. Ward, Edward J. Lewis, Jong Sook Ahn, Christopher N. Johnson, John F. Lyons, Vanessa Martins, Joanne M. Munck, Sharna J. Rich, Tomoko Smyth, Neil T. Thompson, Pamela A. Williams, Nicola E. Wilsher, Nicola G. Wallis, Gianni Chessari
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2018) 17 (7): 1381–1391.
https://doi.org/10.1158/1535-7163.MCT-17-0848
Published: 01 July 2018
View articletitled, ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth
Open the PDF for ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth in another window
Includes: Supplementary data
Journal Articles

Abstract B154: Characterization of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2

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Joanne M. Munck, Valerio Berdini, Luke D. Bevan, Hannah Braithwaite, Ildiko M. Buck, Megan Cassidy, Juan Castro, Aurelie Courtin, James E. Day, Charlotte East, Lynsey Fazal, Brent Graham, Charlotte M. Griffiths-Jones, Tom D. Heightman, Chris J. Hindley, Birikiti Kidane, Justyna Kucia-Tran, John F. Lyons, Vanessa Martins, Sandra Muench, Chris W. Murray, David Norton, Marc O'Reilly, Nick Palmer, Puja Pathuri, Mike Reader, David C. Rees, Sharna J. Rich, Caroline J. Richardson, Harpreet K. Saini, Alpesh Shah, Lukas Stanczuk, Neil T. Thompson, Hugh Walton, Nicola E. Wilsher, Alison J. Woolford, Nicola G. Wallis
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2018) 17 (1_Supplement): B154.
https://doi.org/10.1158/1535-7163.TARG-17-B154
Published: 01 January 2018
View articletitled, Abstract B154: Characterization of a novel ERK1/2 inhibitor, which modulates the phosphorylation and catalytic activity of ERK1/2
Journal Articles

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

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Timothy P.S. Perera, Eleonora Jovcheva, Laurence Mevellec, Jorge Vialard, Desiree De Lange, Tinne Verhulst, Caroline Paulussen, Kelly Van De Ven, Peter King, Eddy Freyne, David C. Rees, Matthew Squires, Gordon Saxty, Martin Page, Christopher W. Murray, Ron Gilissen, George Ward, Neil T. Thompson, David R. Newell, Na Cheng, Liang Xie, Jennifer Yang, Suso J. Platero, Jayaprakash D. Karkera, Christopher Moy, Patrick Angibaud, Sylvie Laquerre, Matthew V. Lorenzi
Journal: Molecular Cancer Therapeutics
Series: Author Choice
Mol Cancer Ther (2017) 16 (6): 1010–1020.
https://doi.org/10.1158/1535-7163.MCT-16-0589
Published: 01 June 2017
View articletitled, Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor
Open the PDF for Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor in another window
Includes: Supplementary data
Journal Articles

Inhibition of HSP90 by AT13387 Delays the Emergence of Resistance to BRAF Inhibitors and Overcomes Resistance to Dual BRAF and MEK Inhibition in Melanoma Models

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Tomoko Smyth, Kim H.T. Paraiso, Keisha Hearn, Ana M. Rodriguez-Lopez, Joanne M. Munck, H. Eirik Haarberg, Vernon K. Sondak, Neil T. Thompson, Mohammad Azab, John F. Lyons, Keiran S.M. Smalley, Nicola G. Wallis
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2014) 13 (12): 2793–2804.
https://doi.org/10.1158/1535-7163.MCT-14-0452
Published: 04 December 2014
View articletitled, Inhibition of HSP90 by AT13387 Delays the Emergence of Resistance to BRAF Inhibitors and Overcomes Resistance to Dual BRAF and MEK Inhibition in Melanoma Models
Open the PDF for Inhibition of HSP90 by AT13387 Delays the Emergence of Resistance to BRAF Inhibitors and Overcomes Resistance to Dual BRAF and MEK Inhibition in Melanoma Models in another window
Journal Articles

The HSP90 Inhibitor, AT13387, Is Effective against Imatinib-Sensitive and -Resistant Gastrointestinal Stromal Tumor Models

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Tomoko Smyth, Thomas Van Looy, Jayne E. Curry, Ana M. Rodriguez-Lopez, Agnieszka Wozniak, Meijun Zhu, Rachel Donsky, Jennifer G. Morgan, Mark Mayeda, Jonathan A. Fletcher, Patrick Schöffski, John Lyons, Neil T. Thompson, Nicola G. Wallis
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2012) 11 (8): 1799–1808.
https://doi.org/10.1158/1535-7163.MCT-11-1046
Published: 08 August 2012
View articletitled, The HSP90 Inhibitor, AT13387, Is Effective against Imatinib-Sensitive and -Resistant Gastrointestinal Stromal Tumor Models
Open the PDF for The HSP90 Inhibitor, AT13387, Is Effective against Imatinib-Sensitive and -Resistant Gastrointestinal Stromal Tumor Models in another window
Includes: Supplementary data
Journal Articles

Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models

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Matthew Squires, George Ward, Gordan Saxty, Valerio Berdini, Anne Cleasby, Peter King, Patrick Angibaud, Tim Perera, Lynsey Fazal, Douglas Ross, Charlotte Griffiths Jones, Andrew Madin, Rajdeep K. Benning, Emma Vickerstaffe, Alistair O'Brien, Martyn Frederickson, Michael Reader, Christopher Hamlett, Michael A. Batey, Sharna Rich, Maria Carr, Darcey Miller, Ruth Feltell, Abarna Thiru, Susanne Bethell, Lindsay A. Devine, Brent L. Graham, Andrew Pike, Jose Cosme, Edward J. Lewis, Eddy Freyne, John Lyons, Julie Irving, Christopher Murray, David R. Newell, Neil T. Thompson
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (9): 1542–1552.
https://doi.org/10.1158/1535-7163.MCT-11-0426
Published: 07 September 2011
View articletitled, Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models
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Includes: Supplementary data
Journal Articles

Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930

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Timothy A. Yap, Mike I. Walton, Lisa-Jane K. Hunter, Melanie Valenti, Alexis de Haven Brandon, Paul D. Eve, Ruth Ruddle, Simon P. Heaton, Alan Henley, Lisa Pickard, Gowri Vijayaraghavan, John J. Caldwell, Neil T. Thompson, Wynne Aherne, Florence I. Raynaud, Suzanne A. Eccles, Paul Workman, Ian Collins, Michelle D. Garrett
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (2): 360–371.
https://doi.org/10.1158/1535-7163.MCT-10-0760
Published: 08 February 2011
View articletitled, Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930
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Includes: Supplementary data
Journal Articles

AT7867 Is a Potent and Oral Inhibitor of AKT and p70 S6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth

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Kyla M. Grimshaw, Lisa-Jane K. Hunter, Timothy A. Yap, Simon P. Heaton, Mike I. Walton, Steven J. Woodhead, Lynsey Fazal, Matthias Reule, Thomas G. Davies, Lisa C. Seavers, Victoria Lock, John F. Lyons, Neil T. Thompson, Paul Workman, Michelle D. Garrett
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2010) 9 (5): 1100–1110.
https://doi.org/10.1158/1535-7163.MCT-09-0986
Published: 09 May 2010
View articletitled, AT7867 Is a Potent and Oral Inhibitor of AKT and p70 S6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth
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Journal Articles

AT7519, a Cyclin-Dependent Kinase Inhibitor, Exerts Its Effects by Transcriptional Inhibition in Leukemia Cell Lines and Patient Samples

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Matthew S. Squires, Laurence Cooke, Victoria Lock, Wenqing Qi, E. Jonathan Lewis, Neil T. Thompson, John F. Lyons, Daruka Mahadevan
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2010) 9 (4): 920–928.
https://doi.org/10.1158/1535-7163.MCT-09-1071
Published: 07 April 2010
View articletitled, AT7519, a Cyclin-Dependent Kinase Inhibitor, Exerts Its Effects by Transcriptional Inhibition in Leukemia Cell Lines and Patient Samples
Open the PDF for AT7519, a Cyclin-Dependent Kinase Inhibitor, Exerts Its Effects by Transcriptional Inhibition in Leukemia Cell Lines and Patient Samples in another window
Journal Articles

Abstract A1: The physiological form of MetAP2 can be inhibited through binding to either of the two active‐site metals

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Nicola G. Wallis, Valerio Berdini, Gilbert Besong, Gianni Chessari, Joe Coyle, Brent Graham, Andrew Madin, Alistair O'Brien, Caroline J. Richardson, Kirsten Smith, Neil T. Thompson, Mladen Vinkovic, Pamela A. Williams
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2009) 8 (12_Supplement): A1.
https://doi.org/10.1158/1535-7163.TARG-09-A1
Published: 10 December 2009
View articletitled, Abstract A1: The physiological form of MetAP2 can be inhibited through binding to either of the two active‐site metals
Journal Articles

Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines

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Matthew S. Squires, Ruth E. Feltell, Nicola G. Wallis, E. Jonathan Lewis, Donna-Michelle Smith, David M. Cross, John F. Lyons, Neil T. Thompson
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2009) 8 (2): 324–332.
https://doi.org/10.1158/1535-7163.MCT-08-0890
Published: 11 February 2009
View articletitled, Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines
Open the PDF for Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines in another window
Includes: Supplementary data