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Page 1
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Richardson CM, Nunns CL, Williamson DS, Parratt MJ, Dokurno P, Howes R, Borgognoni J, Drysdale MJ, Finch H, Hubbard RE, Jackson PS, Kierstan P, Lentzen G, Moore JD, Murray JB, Simmonite H, Surgenor AE, Torrance CJ. Richardson CM, et al. Among authors: borgognoni j. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3880-5. doi: 10.1016/j.bmcl.2007.04.110. Epub 2007 May 6. Bioorg Med Chem Lett. 2007. PMID: 17570665
Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
Richardson CM, Williamson DS, Parratt MJ, Borgognoni J, Cansfield AD, Dokurno P, Francis GL, Howes R, Moore JD, Murray JB, Robertson A, Surgenor AE, Torrance CJ. Richardson CM, et al. Among authors: borgognoni j. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7. doi: 10.1016/j.bmcl.2005.11.048. Epub 2005 Dec 1. Bioorg Med Chem Lett. 2006. PMID: 16325401
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: borgognoni j. 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: borgognoni j. 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: borgognoni j. J Med Chem. 2009 Aug 13;52(15):4794-809. doi: 10.1021/jm900357y. J Med Chem. 2009. PMID: 19610616
Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
Macias AT, Williamson DS, Allen N, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Francis GL, Graham CJ, Howes R, Matassova N, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ. Macias AT, et al. Among authors: borgognoni j. J Med Chem. 2011 Jun 23;54(12):4034-41. doi: 10.1021/jm101625x. Epub 2011 May 20. J Med Chem. 2011. PMID: 21526763
Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked.
Scrace SF, Kierstan P, Borgognoni J, Wang LZ, Denny S, Wayne J, Bentley C, Cansfield AD, Jackson PS, Lockie AM, Curtin NJ, Newell DR, Williamson DS, Moore JD. Scrace SF, et al. Among authors: borgognoni j. Cell Cycle. 2008 Dec 15;7(24):3898-907. doi: 10.4161/cc.7.24.7345. Epub 2008 Dec 4. Cell Cycle. 2008. PMID: 19066469