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Paul Workman
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Journal Articles

Abstract IA014: From targeted phenotypic screen to NXP800: A clinical stage activator of the integrated stress response for the treatment of ARID1A-mutated ovarian carcinoma

Free
Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): IA014.
https://doi.org/10.1158/1535-7163.TARG-23-IA014
Published: 01 December 2023
View articletitled, Abstract IA014: From targeted phenotypic screen to NXP800: A clinical stage activator of the integrated stress response for the treatment of ARID1A-mutated ovarian carcinoma
Journal Articles

Abstract B044: Results of a phase 1 dose escalation clinical trial of NXP800, a novel GCN2 activator, in patients with advanced or metastatic solid tumors

Free
Udai Banerji, Simon Pacey, Karen Finkelstein, Simon Rodney, Ana Filipa Palma DosReis, Giovanni Codaccipisanelli, Mark Sloan, Florence I Raynaud, Ruth Ruddle, Karen Swales, Matthew Tall, Shay Shemesh, Diane Marsolini, Megan Sardone, Justin Hay, Robin Bliss, Enrique Poradosu, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2023) 22 (12_Supplement): B044.
https://doi.org/10.1158/1535-7163.TARG-23-B044
Published: 01 December 2023
View articletitled, Abstract B044: Results of a phase 1 dose escalation clinical trial of NXP800, a novel GCN2 activator, in patients with advanced or metastatic solid tumors
Journal Articles

Abstract LB-C01: The kinase polypharmacology landscape of clinical PARP inhibitors

Free
Albert A Antolin, Malaka Ameratunga, Udai Banerji, Paul Clarke, Paul Workman, Bissan Al-Lazikani
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2019) 18 (12_Supplement): LB-C01.
https://doi.org/10.1158/1535-7163.TARG-19-LB-C01
Published: 01 December 2019
View articletitled, Abstract LB-C01: The kinase polypharmacology landscape of clinical PARP inhibitors
Journal Articles

Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer

Free
Olajumoke O. Popoola, Maria J. Ortiz-Ruiz, Konstantinos Mitsopoulos, Aurelie Mallinger, Robert Te-Poele, Kai Schiemann, Paul Workman, Dirk Wienke, Julian Blagg, Suzanne A. Eccles, Paul A. Clarke
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2018) 17 (1_Supplement): A187.
https://doi.org/10.1158/1535-7163.TARG-17-A187
Published: 01 January 2018
View articletitled, Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer
Journal Articles

Abstract A024: Probe Miner: objective, quantitative, data-driven assessment of chemical probes for target validation

Free
Albert A. Antolin, Joe E. Tym, Angeliki Komianou, Ian Collins, Paul Workman, Bissan Al-Lazikani
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2018) 17 (1_Supplement): A024.
https://doi.org/10.1158/1535-7163.TARG-17-A024
Published: 01 January 2018
View articletitled, Abstract A024: Probe Miner: objective, quantitative, data-driven assessment of chemical probes for target validation
Journal Articles

Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma

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Joo Ern Ang, Akos Pal, Yasmin J. Asad, Alan T. Henley, Melanie Valenti, Gary Box, Alexis de haven Brandon, Victoria L. Revell, Debra J. Skene, Miro Venturi, Ruediger Rueger, Valerie Meresse, Suzanne A. Eccles, Johann S. de Bono, Stanley B. Kaye, Paul Workman, Udai Banerji, Florence I. Raynaud
Journal: Molecular Cancer Therapeutics
Series: Author Choice
Mol Cancer Ther (2017) 16 (10): 2315–2323.
https://doi.org/10.1158/1535-7163.MCT-16-0881
Published: 02 October 2017
View articletitled, Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma
Open the PDF for Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma in another window
Includes: Supplementary data
Journal Articles

The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate–Lactate Exchange in BRAF-Mutant Human Melanoma Cells

Free
Teresa Delgado-Goni, Maria Falck Miniotis, Slawomir Wantuch, Harold G. Parkes, Richard Marais, Paul Workman, Martin O. Leach, Mounia Beloueche-Babari
Journal: Molecular Cancer Therapeutics
Series: Author Choice
Mol Cancer Ther (2016) 15 (12): 2987–2999.
https://doi.org/10.1158/1535-7163.MCT-16-0068
Published: 01 December 2016
View articletitled, The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate–Lactate Exchange in BRAF-Mutant Human Melanoma Cells
Open the PDF for The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate–Lactate Exchange in BRAF-Mutant Human Melanoma Cells in another window
Includes: Supplementary data
Journal Articles

Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation

Free
Joo Ern Ang, Rupinder Pandher, Joo Chew Ang, Yasmin J. Asad, Alan T. Henley, Melanie Valenti, Gary Box, Alexis de Haven Brandon, Richard D. Baird, Lori Friedman, Mika Derynck, Bart Vanhaesebroeck, Suzanne A. Eccles, Stan B. Kaye, Paul Workman, Johann S. de Bono, Florence I. Raynaud
Journal: Molecular Cancer Therapeutics
Series: Author Choice
Mol Cancer Ther (2016) 15 (6): 1412–1424.
https://doi.org/10.1158/1535-7163.MCT-15-0815
Published: 02 June 2016
View articletitled, Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation
Open the PDF for Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation in another window
Includes: Supplementary data
Journal Articles

Abstract B166: A RNA helicase siRNA screen to identify potential therapeutic targets in castration-resistant prostate cancer

Free
Hannah Wang, Emmanuel de Billy, Johann de Bono, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2015) 14 (12_Supplement_2): B166.
https://doi.org/10.1158/1535-7163.TARG-15-B166
Published: 01 December 2015
View articletitled, Abstract B166: A RNA helicase siRNA screen to identify potential therapeutic targets in castration-resistant prostate cancer
Journal Articles

Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology

Free
Paul A. Clarke, Trevor Dale, Christina Esdar, Dennis Waalboer, Olajumoke Adeniji-Popoola, Maria-Jesus Ortiz-Ruiz, Aurelie Mallinger, Ken Ewan, Robert te Poele, Sharon Gowan, Paul Workman, Kai Schiemann, Suzanne A. Eccles, Dirk Wienke, Julian Blagg
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2015) 14 (12_Supplement_2): PR02.
https://doi.org/10.1158/1535-7163.TARG-15-PR02
Published: 01 December 2015
View articletitled, Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology
Journal Articles

The Association of PI3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer

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Craig P. Carden, Adam Stewart, Parames Thavasu, Emma Kipps, Lorna Pope, Mateus Crespo, Susana Miranda, Gerhardt Attard, Michelle D. Garrett, Paul A. Clarke, Paul Workman, Johann S. de Bono, Martin Gore, Stan B Kaye, Udai Banerji
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2012) 11 (7): 1609–1617.
https://doi.org/10.1158/1535-7163.MCT-11-0996
Published: 05 July 2012
View articletitled, The Association of PI3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer
Open the PDF for The Association of PI3 Kinase Signaling and Chemoresistance in Advanced Ovarian Cancer in another window
Includes: Supplementary data
Journal Articles

Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia.

Free
Andrew Moore, Amir Faisal, Vassilios Bavetsias, David Gonzalez de Castro, Chongbo Sun, Butrus Atrash, Melanie Valenti, Alexis de Haven Brandon, Sian Avery, Andrew Pearson, Paul Workman, Julian Blagg, Florence Raynaud, Suzanne Eccles, Spiros Linardopoulos
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (11_Supplement): B74.
https://doi.org/10.1158/1535-7163.TARG-11-B74
Published: 12 November 2011
View articletitled, Abstract B74: The dual FLT3-Aurora inhibitor CCT241736 overcomes resistance to selective FLT3 inhibition driven by FLT3 ligand and FLT3 point mutations in acute myeloid leukemia.
Journal Articles

Abstract B99: Targeting TPR cochaperones of the Hsp90 molecular chaperone complex for specific inhibition.

Free
John F. Darby, Lewis Vidler, Pete J. Simpson, Swee Sharp, Chris Prodromou, Steve Matthews, Swen Hoelder, Laurence Pearl, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (11_Supplement): B99.
https://doi.org/10.1158/1535-7163.TARG-11-B99
Published: 12 November 2011
View articletitled, Abstract B99: Targeting TPR cochaperones of the Hsp90 molecular chaperone complex for specific inhibition.
Journal Articles

Discovering and Developing PI3 Kinase Inhibitors for Cancer: Rapid Progress through Academic-Biotech-Pharma Interactions

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Florence I. Raynaud, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (11): 2017–2018.
https://doi.org/10.1158/1535-7163.MCT-11-0739
Published: 08 November 2011
View articletitled, Discovering and Developing PI3 Kinase Inhibitors for Cancer: Rapid Progress through Academic-Biotech-Pharma Interactions
Open the PDF for Discovering and Developing PI3 Kinase Inhibitors for Cancer: Rapid Progress through Academic-Biotech-Pharma Interactions in another window
Journal Articles

The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo

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Amir Faisal, Lynsey Vaughan, Vassilios Bavetsias, Chongbo Sun, Butrus Atrash, Sian Avery, Yann Jamin, Simon P. Robinson, Paul Workman, Julian Blagg, Florence I. Raynaud, Suzanne A. Eccles, Louis Chesler, Spiros Linardopoulos
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2011) 10 (11): 2115–2123.
https://doi.org/10.1158/1535-7163.MCT-11-0333
Published: 08 November 2011
View articletitled, The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo
Open the PDF for The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo in another window
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
Open the PDF for Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930 in another window
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
Open the PDF for AT7867 Is a Potent and Oral Inhibitor of AKT and p70 S6 Kinase That Induces Pharmacodynamic Changes and Inhibits Human Tumor Xenograft Growth in another window
Journal Articles

Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma

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Nathalie Gaspar, Swee Y. Sharp, Suzanne A. Eccles, Sharon Gowan, Sergey Popov, Chris Jones, Andrew Pearson, Gilles Vassal, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2010) 9 (5): 1219–1233.
https://doi.org/10.1158/1535-7163.MCT-09-0683
Published: 09 May 2010
View articletitled, Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma
Open the PDF for Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma in another window
Includes: Supplementary data
Journal Articles

Abstract B83: Modulation of the HSP90 cochaperone carboxy‐terminus HSC70‐interacting protein (CHIP) increases cellular sensitivity to heat shock protein 90 (HSP90) inhibition

Free
Edward G. Hughes, Swee Y. Sharp, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2009) 8 (12_Supplement): B83.
https://doi.org/10.1158/1535-7163.TARG-09-B83
Published: 10 December 2009
View articletitled, Abstract B83: Modulation of the HSP90 cochaperone carboxy‐terminus HSC70‐interacting protein (CHIP) increases cellular sensitivity to heat shock protein 90 (HSP90) inhibition
Journal Articles

Abstract C7: Sensitization of human colorectal cancer cells to TRAIL induced‐apoptosis following inhibition of PI3K or HSP90

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Grazia Saturno, Paul A. Clarke, Paul Workman
Journal: Molecular Cancer Therapeutics
Mol Cancer Ther (2009) 8 (12_Supplement): C7.
https://doi.org/10.1158/1535-7163.TARG-09-C7
Published: 10 December 2009
View articletitled, Abstract C7: Sensitization of human colorectal cancer cells to TRAIL induced‐apoptosis following inhibition of PI3K or HSP90