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The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
Cheung KM, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P. Cheung KM, et al. Among authors: aherne gw. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. doi: 10.1016/j.bmcl.2005.05.046. Bioorg Med Chem Lett. 2005. PMID: 15955698
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.
Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E. Collins I, et al. Among authors: aherne gw. Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. doi: 10.1016/j.bmc.2005.09.055. Epub 2005 Oct 24. Bioorg Med Chem. 2006. PMID: 16249095
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I. Caldwell JJ, et al. Among authors: aherne gw. J Med Chem. 2008 Apr 10;51(7):2147-57. doi: 10.1021/jm701437d. Epub 2008 Mar 18. J Med Chem. 2008. PMID: 18345609
Identification of inhibitors of checkpoint kinase 1 through template screening.
Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, Collins I. Matthews TP, et al. Among authors: aherne gw. J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j. J Med Chem. 2009. PMID: 19572549
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Reader JC, et al. Among authors: aherne gw. J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22111927 Free PMC article.
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
Matthews TP, McHardy T, Klair S, Boxall K, Fisher M, Cherry M, Allen CE, Addison GJ, Ellard J, Aherne GW, Westwood IM, van Montfort R, Garrett MD, Reader JC, Collins I. Matthews TP, et al. Among authors: aherne gw. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4045-9. doi: 10.1016/j.bmcl.2010.05.096. Epub 2010 May 27. Bioorg Med Chem Lett. 2010. PMID: 20561787
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Garrett MD, Collins I. Lainchbury M, et al. Among authors: aherne gw. J Med Chem. 2012 Nov 26;55(22):10229-40. doi: 10.1021/jm3012933. Epub 2012 Oct 19. J Med Chem. 2012. PMID: 23082860 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: aherne gw. Mol Cancer Ther. 2005 Oct;4(10):1521-32. doi: 10.1158/1535-7163.MCT-05-0135. Mol Cancer Ther. 2005. PMID: 16227401
136 results