The acetylation of lysine residues of histone and nonhistone proteins is a post-translational modification catalysed by the so-called histone acetyltransferases (HATs) that plays a crucial role in several biological settings. The deregulation of this enzymatic activity is implicated in many disease conditions such as cancer and inflammatory and neurological disorders. Despite many histone acetyltransferase inhibitors (HATi) have been identified so far, there is still the need for new, metabolically stable, more potent and selective HATi as potential therapeutic agents and/or as chemical tools for studying HAT biology. In the present chapter, the main features of HAT enzymes and related diseases have been summarized, with a particular focus on HATi, analysing their structure-activity relationships, mechanisms of action and potential therapeutic applications.

Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors / Trisciuoglio, Daniela; Rotili, Dante. - (2019), pp. 1-30. - TOPICS IN MEDICINAL CHEMISTRY. [10.1007/7355_2019_71].

Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors

Rotili, Dante
2019

Abstract

The acetylation of lysine residues of histone and nonhistone proteins is a post-translational modification catalysed by the so-called histone acetyltransferases (HATs) that plays a crucial role in several biological settings. The deregulation of this enzymatic activity is implicated in many disease conditions such as cancer and inflammatory and neurological disorders. Despite many histone acetyltransferase inhibitors (HATi) have been identified so far, there is still the need for new, metabolically stable, more potent and selective HATi as potential therapeutic agents and/or as chemical tools for studying HAT biology. In the present chapter, the main features of HAT enzymes and related diseases have been summarized, with a particular focus on HATi, analysing their structure-activity relationships, mechanisms of action and potential therapeutic applications.
2019
Topics in medicinal chemistry
Cancer; Chemical probes; Epigenetics; Histone acetyltransferase inhibitors; Structure- and ligand-based drug discovery
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Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors / Trisciuoglio, Daniela; Rotili, Dante. - (2019), pp. 1-30. - TOPICS IN MEDICINAL CHEMISTRY. [10.1007/7355_2019_71].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1355619
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