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Small Molecule Inhibitor Publications

Cheng D, Valente S, Castellano S, Sbardella G, Di Santo R, Costi R, Bedford MT, Mai A. Novel 3,5-bis(bromogydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: Enzyme selectivity and cellular activity. J Med Chem 54(13):4928-4932, 2011.


Bissinger EM, Heinke R, Spannhoff A, Eberlin A, Metzger E, Cura V, Hassenboehler P, Cavarelli J, Schüle R, Bedford MT, Sippl W, Jung M. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. Bioorg Med Chem. 2011 Mar 24.


Spannhoff A, Kim YK, Raynal NJ, Gharibyan V, Su MB, Zhou YY, Li J, Castellano S, Sbardella G, Issa JP, Bedford MT. Histone deacetylase inhibitor activity in royal jelly might facilitate caste switching in bees. EMBO Rep. 2011 Mar;12(3):238-43.


Cheng D, Bedford MT. Xenoestrogens Regulate the Activity of Arginine Methyltransferases.Chembiochem. 2011 Jan 24;12(2):323-9.


Chang Y, Ganesh T, Horton JR, Spannhoff A, Liu J, Sun A, Zhang X, Bedford MT, Shinkai Y, Snyder JP, Cheng X. Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases. J Mol Biol. 2010 Jul 2;400(1):1-7. Epub 2010 Apr 29.


Castellano S, Milite C, Ragno R, Simeoni S, Mai A, Limongelli V, Novellino E, Bauer I, Brosch G, Spannhoff A, Cheng D, Bedford MT, Sbardella G. Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1). ChemMedChem. 2010 Mar 1;5(3):398-414.


Chang Y, Zhang X, Horton JR, Spannhoff A, Bedford MT, Cheng S. Structural basis for inhibition of G9a and GLP histone lysine methyltransferases by BIX-01294. Nat Struct Mol Biol. e-Pub 2/2009.


Mai A, Cheng D, Bedford MT, Valente S, Nebbioso A, Perrone A, Brosch G, Sbardella G, De Bellis F, Miceli M, Altucci L. Epigenetic multiple ligands: Mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors. J Med Chem 51:2279-2290, 2008.


Mai A, Valente S, Cheng D, Perrone A, Ragno R, Simeoni S, Sbardella G, Brosch G, Nebbioso A, Conte M, Altucci L, and Bedford MT. Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors. Chem Med Chem 2:987-991, 2007.


Cheng D, Yadav N, King RW, Swanson MS, Weinstein EJ, Bedford MT. Small molecule regulators of protein arginine methyltransferases. J Biol Chem 279:23892-23899, 2004.


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