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Page 1
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Brown AR, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, Elmore MA, Firth A, Goodwin R, Goutcher S, Grant E, Grassie M, Grove SJ, Hamilton NM, Hampson H, Hillier A, Ho KK, Kiczun M, Kingsbury C, Kultgen SG, Littlewood PT, Lusher SJ, Macdonald S, McIntosh L, McIntyre T, Mistry A, Morphy JR, Nimz O, Ohlmeyer M, Pick J, Rankovic Z, Sherborne B, Smith A, Speake M, Spinks G, Thomson F, Watson L, Weston M. Brown AR, et al. Among authors: sherborne b. Bioorg Med Chem Lett. 2011 Jan 1;21(1):137-40. doi: 10.1016/j.bmcl.2010.11.054. Epub 2010 Nov 16. Bioorg Med Chem Lett. 2011. PMID: 21129964
Murgocil is a highly bioactive staphylococcal-specific inhibitor of the peptidoglycan glycosyltransferase enzyme MurG.
Mann PA, Müller A, Xiao L, Pereira PM, Yang C, Ho Lee S, Wang H, Trzeciak J, Schneeweis J, Dos Santos MM, Murgolo N, She X, Gill C, Balibar CJ, Labroli M, Su J, Flattery A, Sherborne B, Maier R, Tan CM, Black T, Onder K, Kargman S, Monsma FJ Jr, Pinho MG, Schneider T, Roemer T. Mann PA, et al. Among authors: sherborne b. ACS Chem Biol. 2013 Nov 15;8(11):2442-51. doi: 10.1021/cb400487f. Epub 2013 Sep 5. ACS Chem Biol. 2013. PMID: 23957438
Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.
Kosugi T, Mitchell DR, Fujino A, Imai M, Kambe M, Kobayashi S, Makino H, Matsueda Y, Oue Y, Komatsu K, Imaizumi K, Sakai Y, Sugiura S, Takenouchi O, Unoki G, Yamakoshi Y, Cunliffe V, Frearson J, Gordon R, Harris CJ, Kalloo-Hosein H, Le J, Patel G, Simpson DJ, Sherborne B, Thomas PS, Suzuki N, Takimoto-Kamimura M, Kataoka K. Kosugi T, et al. Among authors: sherborne b. J Med Chem. 2012 Aug 9;55(15):6700-15. doi: 10.1021/jm300411k. Epub 2012 Jul 31. J Med Chem. 2012. PMID: 22746295
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ. Ray P, et al. Among authors: sherborne b. Bioorg Med Chem Lett. 2011 Jan 1;21(1):97-101. doi: 10.1016/j.bmcl.2010.11.060. Epub 2010 Nov 19. Bioorg Med Chem Lett. 2011. PMID: 21145740
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. Seganish WM, et al. Among authors: sherborne b. ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288698 Free PMC article.
NanoClick: A High Throughput, Target-Agnostic Peptide Cell Permeability Assay.
Peier A, Ge L, Boyer N, Frost J, Duggal R, Biswas K, Edmondson S, Hermes JD, Yan L, Zimprich C, Sadruddin A, Kristal Kaan HY, Chandramohan A, Brown CJ, Thean D, Lee XE, Yuen TY, Ferrer-Gago FJ, Johannes CW, Lane DP, Sherborne B, Corona C, Robers MB, Sawyer TK, Partridge AW. Peier A, et al. Among authors: sherborne b. ACS Chem Biol. 2021 Feb 19;16(2):293-309. doi: 10.1021/acschembio.0c00804. Epub 2021 Feb 4. ACS Chem Biol. 2021. PMID: 33539064
Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Ray P, et al. Among authors: sherborne b. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21251828
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.
Deng Q, Lim YH, Anand R, Yu Y, Kim JH, Zhou W, Zheng J, Tempest P, Levorse D, Zhang X, Greene S, Mullins D, Culberson C, Sherborne B, Parker EM, Stamford A, Ali A. Deng Q, et al. Among authors: sherborne b. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2958-62. doi: 10.1016/j.bmcl.2015.05.036. Epub 2015 May 21. Bioorg Med Chem Lett. 2015. PMID: 26048804
39 results