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Allan E. Surgenor
Researcher at Institute of Cancer Research
Publications - 34
Citations - 3687
Allan E. Surgenor is an academic researcher from Institute of Cancer Research. The author has contributed to research in topics: Docking (molecular) & Pyrazole. The author has an hindex of 22, co-authored 34 publications receiving 3221 citations.
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Journal ArticleDOI
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models
András Kotschy,Szlávik Zoltán,James A. H. Murray,James Edward Paul Davidson,Ana Leticia Maragno,Gaëtane Le Toumelin-Braizat,Maïa Chanrion,Gemma L. Kelly,Gemma L. Kelly,Jia-Nan Gong,Jia-Nan Gong,Donia M Moujalled,Alain Bruno,Csékei Márton,Attila Paczal,Zoltán B. Szabó,Szabolcs Sipos,Gabor Radics,Proszenyák Ágnes,Balázs Bálint,Levente Ondi,Gábor Blasko,Alan P. Robertson,Allan E. Surgenor,Pawel Dokurno,Chen I-Jen,Natalia Matassova,Julia Smith,C. Pedder,Chris Graham,Aurélie Studeny,Gaëlle Lysiak-Auvity,Anne-Marie Girard,Fabienne Gravé,David J. Segal,David J. Segal,Chris D. Riffkin,Chris D. Riffkin,Giovanna Pomilio,Laura C. A. Galbraith,Laura C. A. Galbraith,Brandon J. Aubrey,Brandon J. Aubrey,Brandon J. Aubrey,Margs S. Brennan,Margs S. Brennan,Marco J Herold,Marco J Herold,Catherine Chang,Catherine Chang,Ghislaine Guasconi,Nicolas Cauquil,Fabien Melchiore,Nolwen Guigal-Stephan,Brian Lockhart,Frédéric Colland,John A. Hickman,Andrew W. Roberts,David C.S. Huang,David C.S. Huang,Andrew H. Wei,Andrew H. Wei,Andreas Strasser,Andreas Strasser,Guillaume Lessene,Guillaume Lessene,Olivier Geneste +66 more
TL;DR: It is demonstrated that S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway.
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
Identification of Chemically Diverse Chk1 Inhibitors by Receptor-Based Virtual Screening.
Nicolas Foloppe,Lisa M. Fisher,Rob Howes,Andrew Potter,Alan G.S. Robertson,Allan E. Surgenor +5 more
TL;DR: This work illustrates how virtual screening can identify a diverse set of ligands which bind to the targeted site, and the structural models for these ligands in the Chk1 ATP-binding site will facilitate further medicinal chemistry efforts targeting this kinase.
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.