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Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.
King ON, Li XS, Sakurai M, Kawamura A, Rose NR, Ng SS, Quinn AM, Rai G, Mott BT, Beswick P, Klose RJ, Oppermann U, Jadhav A, Heightman TD, Maloney DJ, Schofield CJ, Simeonov A. King ON, et al. Among authors: heightman td. PLoS One. 2010 Nov 23;5(11):e15535. doi: 10.1371/journal.pone.0015535. PLoS One. 2010. PMID: 21124847 Free PMC article.
Inhibition of histone demethylases by 4-carboxy-2,2'-bipyridyl compounds.
Chang KH, King ONF, Tumber A, Woon ECY, Heightman TD, McDonough MA, Schofield CJ, Rose NR. Chang KH, et al. Among authors: heightman td. ChemMedChem. 2011 May 2;6(5):759-764. doi: 10.1002/cmdc.201100026. Epub 2011 Mar 15. ChemMedChem. 2011. PMID: 21412984 Free PMC article. No abstract available.
A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.
Rooney TP, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S, Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC, Cook A, Paton RS, Müller S, Knapp S, Brennan PE, Conway SJ. Rooney TP, et al. Among authors: heightman td. Angew Chem Int Ed Engl. 2014 Jun 10;53(24):6126-30. doi: 10.1002/anie.201402750. Epub 2014 May 12. Angew Chem Int Ed Engl. 2014. PMID: 24821300 Free PMC article.
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD. Hewings DS, et al. Among authors: heightman td. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
63 results