Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy

Abstract: The term epigenetics is defined as heritable changes in gene expression that are not due to alterations of the DNA sequence. In the last years, it has become more and more evident that dysregulated epigenetic regulatory processes have a central role in cancer onset and progression. In contrast to DNA mutations, epigenetic modifications are reversible and, hence, suitable for pharmacological interventions. Reversible histone methylation is an important process within epigenetic regulation, and the investigation of its role in cancer has led to the identification of lysine methyltransferases and demethylases as promising targets for new anticancer drugs. In this review, we describe those enzymes and their inhibitors that have already reached the first stages of clinical trials in cancer therapy, namely the histone methyltransferases DOT1L and EZH2 as well as the demethylase LSD1.

Keywords

Methylome - Lysine methylation - Histone methyltransferase - Histone demethylase - Clinical trial - Methyltransferase inhibitors - Demethylase inhibitors - Epigenetics - Histone modifications

Standort
Deutsche Nationalbibliothek Frankfurt am Main
Umfang
Online-Ressource
Sprache
Englisch
Anmerkungen
Clinical epigenetics. 8 (2016), 57, DOI 10.1186/s13148-016-0223-4, issn: 1868-7083

Schlagwort
Methyltransferase
Histone
Methoxybenzoat-Monooxygenase
Inhibitor
Epigenetik
Klinisches Experiment
Krebs
Onkologie

Ereignis
Veröffentlichung
(wo)
Freiburg
(wer)
Universität
(wann)
2017
Urheber

DOI
10.1186/s13148-016-0223-4
URN
urn:nbn:de:bsz:25-freidok-126026
Rechteinformation
Kein Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Letzte Aktualisierung
14.08.2025, 10:56 MESZ

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Entstanden

  • 2017

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