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Page 1
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, Howes R, Hubbard RE, James K, Jordan AM, Lockie A, Martins V, Massey A, Matthews TP, McDonald E, Northfield CJ, Pearl LH, Prodromou C, Ray S, Raynaud FI, Roughley SD, Sharp SY, Surgenor A, Walmsley DL, Webb P, Wood M, Workman P, Wright L. Brough PA, et al. Among authors: drysdale mj. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. J Med Chem. 2008. PMID: 18020435
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.
Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Williamson DS, et al. Among authors: drysdale mj. J Med Chem. 2009 Mar 26;52(6):1510-3. doi: 10.1021/jm801627a. J Med Chem. 2009. PMID: 19256508
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.
Brough PA, Barril X, Borgognoni J, Chene P, Davies NG, Davis B, Drysdale MJ, Dymock B, Eccles SA, Garcia-Echeverria C, Fromont C, Hayes A, Hubbard RE, Jordan AM, Jensen MR, Massey A, Merrett A, Padfield A, Parsons R, Radimerski T, Raynaud FI, Robertson A, Roughley SD, Schoepfer J, Simmonite H, Sharp SY, Surgenor A, Valenti M, Walls S, Webb P, Wood M, Workman P, Wright L. Brough PA, et al. Among authors: drysdale mj. J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y. J Med Chem. 2009. PMID: 19610616
A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells.
Massey AJ, Williamson DS, Browne H, Murray JB, Dokurno P, Shaw T, Macias AT, Daniels Z, Geoffroy S, Dopson M, Lavan P, Matassova N, Francis GL, Graham CJ, Parsons R, Wang Y, Padfield A, Comer M, Drysdale MJ, Wood M. Massey AJ, et al. Among authors: drysdale mj. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. doi: 10.1007/s00280-009-1194-3. Epub 2009 Dec 13. Cancer Chemother Pharmacol. 2010. PMID: 20012863
Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.
Davies NG, Browne H, Davis B, Drysdale MJ, Foloppe N, Geoffrey S, Gibbons B, Hart T, Hubbard R, Jensen MR, Mansell H, Massey A, Matassova N, Moore JD, Murray J, Pratt R, Ray S, Robertson A, Roughley SD, Schoepfer J, Scriven K, Simmonite H, Stokes S, Surgenor A, Webb P, Wood M, Wright L, Brough P. Davies NG, et al. Among authors: drysdale mj. Bioorg Med Chem. 2012 Nov 15;20(22):6770-89. doi: 10.1016/j.bmc.2012.08.050. Epub 2012 Sep 4. Bioorg Med Chem. 2012. PMID: 23018093
Structure-based discovery of a new class of Hsp90 inhibitors.
Barril X, Brough P, Drysdale M, Hubbard RE, Massey A, Surgenor A, Wright L. Barril X, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5187-91. doi: 10.1016/j.bmcl.2005.08.092. Epub 2005 Oct 3. Bioorg Med Chem Lett. 2005. PMID: 16202589
Targeting Hsp90 for the treatment of cancer.
Drysdale MJ, Brough PA, Massey A, Jensen MR, Schoepfer J. Drysdale MJ, et al. Curr Opin Drug Discov Devel. 2006 Jul;9(4):483-95. Curr Opin Drug Discov Devel. 2006. PMID: 16889231 Review.
45 results