Issue 4, 2022

Lysine methyltransferase inhibitors: where we are now

Abstract

Protein lysine methyltransferases constitute a large family of epigenetic writers that catalyse the transfer of a methyl group from the cofactor S-adenosyl-L-methionine to histone- and non-histone-specific substrates. Alterations in the expression and activity of these proteins have been linked to the genesis and progress of several diseases, including cancer, neurological disorders, and growing defects, hence they represent interesting targets for new therapeutic approaches. Over the past two decades, the identification of modulators of lysine methyltransferases has increased tremendously, clarifying the role of these proteins in different physio-pathological states. The aim of this review is to furnish an updated outlook about the protein lysine methyltransferases disclosed modulators, reporting their potency, their mechanism of action and their eventual use in clinical and preclinical studies.

Graphical abstract: Lysine methyltransferase inhibitors: where we are now

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Article information

Article type
Review Article
Submitted
08 окт 2021
Accepted
10 дек 2021
First published
13 дек 2021
This article is Open Access
Creative Commons BY-NC license

RSC Chem. Biol., 2022,3, 359-406

Lysine methyltransferase inhibitors: where we are now

A. Feoli, M. Viviano, A. Cipriano, C. Milite, S. Castellano and G. Sbardella, RSC Chem. Biol., 2022, 3, 359 DOI: 10.1039/D1CB00196E

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