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Synthesis and Biological Validation of Novel Synthetic Histone/Protein Methyltransferase Inhibitors

Antonello Mai, Sérgio Valente, Donghang Cheng, Andrea Perrone, Rino Ragno, Silvia Simeoni, Gianluca Sbardella, Gerald Brosch, Angela Nebbioso, Mariarosaria Conte, Lucia Altucci, Mark T. Bedford

Open publisher page 56 citations

Abstract

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).

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What this paper is about

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).

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Available abstract

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).

Key concepts: Methyltransferase, Histone methyltransferase, Epigenetics, Histone, Lysine, Biochemistry, Enzyme, Protein arginine methyltransferase 5

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