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Structure-guided design of purine-based probes for selective Nek2 inhibition.
Coxon CR, Wong C, Bayliss R, Boxall K, Carr KH, Fry AM, Hardcastle IR, Matheson CJ, Newell DR, Sivaprakasam M, Thomas H, Turner D, Yeoh S, Wang LZ, Griffin RJ, Golding BT, Cano C. Coxon CR, et al. Among authors: bayliss r. Oncotarget. 2017 Mar 21;8(12):19089-19124. doi: 10.18632/oncotarget.13249. Oncotarget. 2017. PMID: 27833088 Free PMC article.
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V. Bouloc N, et al. Among authors: bayliss r. Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20833547
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.
Whelligan DK, Solanki S, Taylor D, Thomson DW, Cheung KM, Boxall K, Mas-Droux C, Barillari C, Burns S, Grummitt CG, Collins I, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Whelligan DK, et al. Among authors: bayliss r. J Med Chem. 2010 Nov 11;53(21):7682-98. doi: 10.1021/jm1008727. J Med Chem. 2010. PMID: 20936789 Free PMC article.
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.
Solanki S, Innocenti P, Mas-Droux C, Boxall K, Barillari C, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Solanki S, et al. Among authors: bayliss r. J Med Chem. 2011 Mar 24;54(6):1626-39. doi: 10.1021/jm1011726. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366329
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S. Innocenti P, et al. Among authors: bayliss r. J Med Chem. 2012 Apr 12;55(7):3228-41. doi: 10.1021/jm201683b. Epub 2012 Mar 23. J Med Chem. 2012. PMID: 22404346 Free PMC article.
Cell cycle regulation by the NEK family of protein kinases.
Fry AM, O'Regan L, Sabir SR, Bayliss R. Fry AM, et al. Among authors: bayliss r. J Cell Sci. 2012 Oct 1;125(Pt 19):4423-33. doi: 10.1242/jcs.111195. Epub 2012 Nov 6. J Cell Sci. 2012. PMID: 23132929 Free PMC article. Review.
252 results