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106 results

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Page 1
Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling.
Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW, Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L, Blagg J, Workman P, Garrett MD, Mittnacht S. Stockwell SR, et al. Among authors: blagg j. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568. Epub 2012 Jan 12. PLoS One. 2012. PMID: 22253692 Free PMC article.
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: blagg j. J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j. J Med Chem. 2010. PMID: 20565112
A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription.
Ewan K, Pajak B, Stubbs M, Todd H, Barbeau O, Quevedo C, Botfield H, Young R, Ruddle R, Samuel L, Battersby A, Raynaud F, Allen N, Wilson S, Latinkic B, Workman P, McDonald E, Blagg J, Aherne W, Dale T. Ewan K, et al. Among authors: blagg j. Cancer Res. 2010 Jul 15;70(14):5963-73. doi: 10.1158/0008-5472.CAN-10-1028. Epub 2010 Jul 7. Cancer Res. 2010. PMID: 20610623 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: blagg j. 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
Epigenetics: Targeting leukemia on the DOT.
Travers J, Blagg J, Workman P. Travers J, et al. Among authors: blagg j. Nat Chem Biol. 2011 Aug 28;7(10):663-5. doi: 10.1038/nchembio.661. Nat Chem Biol. 2011. PMID: 21873997 No abstract available.
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. Among authors: blagg j. 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.
Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.
Silva-Santisteban MC, Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, Collins I, Garrett MD, van Montfort RL. Silva-Santisteban MC, et al. Among authors: blagg j. PLoS One. 2013 Jun 12;8(6):e65689. doi: 10.1371/journal.pone.0065689. Print 2013. PLoS One. 2013. PMID: 23776527 Free PMC article.
106 results