M
Martin J. Drysdale
Researcher at Institute of Cancer Research
Publications - 64
Citations - 4417
Martin J. Drysdale is an academic researcher from Institute of Cancer Research. The author has contributed to research in topics: Hsp90 & Heat shock protein. The author has an hindex of 31, co-authored 64 publications receiving 4099 citations. Previous affiliations of Martin J. Drysdale include University of Glasgow & University of Nottingham.
Papers
More filters
Journal ArticleDOI
NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis
Suzanne A. Eccles,Andrew Massey,Florence I. Raynaud,Swee Y. Sharp,Gary Box,Melanie Valenti,Lisa Patterson,Alexis De Haven Brandon,Sharon Gowan,F. E. Boxall,Wynne Aherne,Martin G. Rowlands,Angela Hayes,Vanessa Martins,Frederique Urban,Kathy Boxall,Chrisostomos Prodromou,Laurence H. Pearl,Karen James,Thomas P. Matthews,Kwai-Ming Cheung,Andrew Kalusa,Keith Jones,Edward McDonald,Xavier Barril,Paul Brough,Julie E. Cansfield,Brian Dymock,Martin J. Drysdale,Harry Finch,Rob Howes,Roderick E. Hubbard,Alan Surgenor,Paul Webb,Michael Wood,Lisa Wright,Paul Workman +36 more
TL;DR: The data show that NVP-AUY922 is a potent, novel inhibitor of HSP90, acting via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis.
Journal ArticleDOI
4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer
Paul Brough,Wynne Aherne,Xavier Barril,Jenifer Borgognoni,Kathy Boxall,Julie E. Cansfield,Kwai-Ming J. Cheung,Ian Collins,Nicholas G. M. Davies,Martin J. Drysdale,Brian Dymock,Suzanne A. Eccles,Harry Finch,Alexandra Fink,Angela Hayes,R. Howes,Roderick E. Hubbard,Karen James,Allan M. Jordan,Andrea M. Lockie,Vanessa Martins,Andrew Massey,Thomas P. Matthews,Edward McDonald,Christopher J. Northfield,Laurence H. Pearl,Chrisostomos Prodromou,Stuart C. Ray,Florence I. Raynaud,Stephen D. Roughley,Swee Y. Sharp,Allan E. Surgenor,D. Lee Walmsley,Paul Webb,Michael Wood,Paul Workman,Lisa Wright +36 more
TL;DR: The structure-based design, synthesis, structure-activity relationships and pharmacokinetics of potent small-molecule inhibitors of Hsp90 based on the 4,5-diarylisoxazole scaffold are described and analogues from this series have high affinity for HSp90, as measured in a fluorescence polarization (FP) competitive binding assay, and are active in cancer cell lines.
Journal ArticleDOI
A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells
Andrew Massey,Douglas S. Williamson,Helen Browne,James Brooke Murray,Pawel Dokurno,Terry Shaw,Macias Alba,Zoe Daniels,Stephanie Geoffroy,Melanie Dopson,Paul Lavan,Natalia Matassova,Geraint L. Francis,Christopher John Graham,Rachel Parsons,Yikang Wang,Antony Padfield,Mike Comer,Martin J. Drysdale,Michael Wood +19 more
TL;DR: It is suggested that small molecule inhibitors of Hsc70/Hsp70 phenotypically mimic the cellular mode of action of a small molecule Hsp90 inhibitor and can potentiate the apoptotic potential of asmall molecule HSp90 inhibitor in certain cell lines.
Journal ArticleDOI
Structure-Activity Relationships in Purine-Based Inhibitor Binding to Hsp90 Isoforms
Lisa Wright,Xavier Barril,Brian Dymock,Louisa Sheridan,Allan E. Surgenor,Mandy Beswick,Martin J. Drysdale,Adam Collier,Andrew Massey,Nicholas G. M. Davies,Alex Fink,Christophe Fromont,Wynne Aherne,Kathy Boxall,Swee Y. Sharp,Paul Workman,Roderick E. Hubbard +16 more
TL;DR: The structures of the HSP90alpha N-terminal domain complexed with the purine-based inhibitor, PU3, and analogs with enhanced potency both in enzyme and cell-based assays confirm that the molecules inhibit cell growth by a mechanism dependent on H SP90 inhibition.
Journal ArticleDOI
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Brian Dymock,Xavier Barril,Paul Brough,Julie E. Cansfield,Andrew Massey,Edward McDonald,Roderick E. Hubbard,Allan E. Surgenor,Stephen D. Roughley,Paul Webb,Paul Workman,Lisa Wright,Martin J. Drysdale +12 more
TL;DR: The crystal structure of a previously reported screening hit 1 (CCT018159) bound to the N terminal domain of molecular chaperone Hsp90 has been used to design 5-amide analogues that exhibit enhanced potency against the target in binding and functional assays with accompanying appropriate cellular pharmacodynamic changes.