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.
Trisciuoglio, D., Rotili, D. (2019). Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors. In Topics in medicinal chemistry (pp. 1-30). Springer Nature [10.1007/7355_2019_71].
Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors
Rotili, Dante
2019-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
