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Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB. Sleebs BE, et al. Among authors: yang h. J Med Chem. 2011 Mar 24;54(6):1914-26. doi: 10.1021/jm101596e. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366295
Structure-guided design of a selective BCL-X(L) inhibitor.
Lessene G, Czabotar PE, Sleebs BE, Zobel K, Lowes KN, Adams JM, Baell JB, Colman PM, Deshayes K, Fairbrother WJ, Flygare JA, Gibbons P, Kersten WJ, Kulasegaram S, Moss RM, Parisot JP, Smith BJ, Street IP, Yang H, Huang DC, Watson KG. Lessene G, et al. Among authors: yang h. Nat Chem Biol. 2013 Jun;9(6):390-7. doi: 10.1038/nchembio.1246. Epub 2013 Apr 21. Nat Chem Biol. 2013. PMID: 23603658
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: yang h. 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 Development of Potent Benzoylurea Inhibitors of BCL-XL and BCL-2.
Roy MJ, Vom A, Okamoto T, Smith BJ, Birkinshaw RW, Yang H, Abdo H, White CA, Segal D, Huang DCS, Baell JB, Colman PM, Czabotar PE, Lessene G. Roy MJ, et al. Among authors: yang h. J Med Chem. 2021 May 13;64(9):5447-5469. doi: 10.1021/acs.jmedchem.0c01771. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904752
Further insights into the effects of pre-organizing the BimBH3 helix.
Okamoto T, Segal D, Zobel K, Fedorova A, Yang H, Fairbrother WJ, Huang DC, Smith BJ, Deshayes K, Czabotar PE. Okamoto T, et al. Among authors: yang h. ACS Chem Biol. 2014 Mar 21;9(3):838-9. doi: 10.1021/cb400638p. Epub 2014 Feb 18. ACS Chem Biol. 2014. PMID: 24547872 No abstract available.
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: yang h. J Biomol Screen. 2011 Dec;16(10):1196-205. doi: 10.1177/1087057111421631. Epub 2011 Nov 14. J Biomol Screen. 2011. PMID: 22086725
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