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Page 1
Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S. Hatch SB, et al. Among authors: raynaud f. Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017. Epigenetics Chromatin. 2017. PMID: 28265301 Free PMC article.
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity.
Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V, Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW. Stimson L, et al. Among authors: raynaud fi. Mol Cancer Ther. 2005 Oct;4(10):1521-32. doi: 10.1158/1535-7163.MCT-05-0135. Mol Cancer Ther. 2005. PMID: 16227401
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.
Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E. Bavetsias V, et al. Among authors: raynaud fi. J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j. J Med Chem. 2010. PMID: 20565112
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.
Wilson SC, Atrash B, Barlow C, Eccles S, Fischer PM, Hayes A, Kelland L, Jackson W, Jarman M, Mirza A, Moreno J, Nutley BP, Raynaud FI, Sheldrake P, Walton M, Westwood R, Whittaker S, Workman P, McDonald E. Wilson SC, et al. Bioorg Med Chem. 2011 Nov 15;19(22):6949-65. doi: 10.1016/j.bmc.2011.08.051. Epub 2011 Aug 31. Bioorg Med Chem. 2011. PMID: 21982796
Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.
Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S. Moore AS, et al. Among authors: raynaud fi. Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52. Epub 2012 Feb 22. Leukemia. 2012. PMID: 22354205 Free PMC article.
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.
Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, Raynaud FI, Workman P, Eccles SA, Bayliss R, Linardopoulos S, Blagg J. Bavetsias V, et al. J Med Chem. 2012 Oct 25;55(20):8721-34. doi: 10.1021/jm300952s. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 23043539 Free PMC article.
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.
Bavetsias V, Faisal A, Crumpler S, Brown N, Kosmopoulou M, Joshi A, Atrash B, Pérez-Fuertes Y, Schmitt JA, Boxall KJ, Burke R, Sun C, Avery S, Bush K, Henley A, Raynaud FI, Workman P, Bayliss R, Linardopoulos S, Blagg J. Bavetsias V, et al. J Med Chem. 2013 Nov 27;56(22):9122-35. doi: 10.1021/jm401115g. Epub 2013 Nov 6. J Med Chem. 2013. PMID: 24195668 Free PMC article.
341 results