(Chemical Equation Presented) Coding control: Protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) are epigenetic enzymes involved in regulation of gene expression and cellular processes. A new series of histone/protein methyltransferase inhibitors based on the 1,5-diphenyl-1,4-pentadien-3-one scaffold is reported. The described compounds showed various degrees of selectivity against the tested PRMTs (PRMT1 and CARM1) and HKMT (SET7). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors / Mai, Antonello; Valente, Sergio; Donghang, Cheng; Andrea, Perrone; Ragno, Rino; Simeoni, Silvia; Gianluca, Sbardella; Gerald, Brosch; Mark t, Bedford. - In: CHEMMEDCHEM. - ISSN 1860-7179. - STAMPA. - 2:7(2007), pp. 987-991. [10.1002/cmdc.200700023]
Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors
MAI, Antonello;VALENTE, Sergio;RAGNO, Rino;SIMEONI, silvia;
2007
Abstract
(Chemical Equation Presented) Coding control: Protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) are epigenetic enzymes involved in regulation of gene expression and cellular processes. A new series of histone/protein methyltransferase inhibitors based on the 1,5-diphenyl-1,4-pentadien-3-one scaffold is reported. The described compounds showed various degrees of selectivity against the tested PRMTs (PRMT1 and CARM1) and HKMT (SET7). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
