TY - CHAP
T1 - Histone Acetyltransferase Enzymes
T2 - From Biological Implications to Most Relevant Inhibitors
AU - Trisciuoglio, Daniela
AU - Rotili, Dante
N1 - Publisher Copyright:
© 2019, Springer Nature Switzerland AG.
Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020
Y1 - 2020
N2 - 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.
AB - 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.
KW - Cancer
KW - Chemical probes
KW - Epigenetics
KW - Histone acetyltransferase inhibitors
KW - Structure- and ligand-based drug discovery
UR - http://www.scopus.com/inward/record.url?scp=85083989062&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85083989062&partnerID=8YFLogxK
U2 - 10.1007/7355_2019_71
DO - 10.1007/7355_2019_71
M3 - Chapter
AN - SCOPUS:85083989062
T3 - Topics in Medicinal Chemistry
SP - 93
EP - 122
BT - Topics in Medicinal Chemistry
PB - Springer
ER -