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Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G. Sleebs BE, et al. Among authors: nikolakopoulos g. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.
Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G. Koehler MF, et al. Among authors: nikolakopoulos g. ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944740 Free PMC article.
An efficient high-throughput screening method for MYST family acetyltransferases, a new class of epigenetic drug targets.
Falk H, Connor T, Yang H, Loft KJ, Alcindor JL, Nikolakopoulos G, Surjadi RN, Bentley JD, Hattarki MK, Dolezal O, Murphy JM, Monahan BJ, Peat TS, Thomas T, Baell JB, Parisot JP, Street IP. Falk H, et al. Among authors: nikolakopoulos g. J Biomol Screen. 2011 Dec;16(10):1196-205. doi: 10.1177/1087057111421631. Epub 2011 Nov 14. J Biomol Screen. 2011. PMID: 22086725
Euodenine A: a small-molecule agonist of human TLR4.
Neve JE, Wijesekera HP, Duffy S, Jenkins ID, Ripper JA, Teague SJ, Campitelli M, Garavelas A, Nikolakopoulos G, Le PV, de A Leone P, Pham NB, Shelton P, Fraser N, Carroll AR, Avery VM, McCrae C, Williams N, Quinn RJ. Neve JE, et al. Among authors: nikolakopoulos g. J Med Chem. 2014 Feb 27;57(4):1252-75. doi: 10.1021/jm401321v. Epub 2014 Feb 7. J Med Chem. 2014. PMID: 24471857
17 results