Human DNA (cytosine-5)-methyltransferases: A functional and structural perspective for epigenetic cancer therapy

Publication date: Available online 6 June 2017
Source:Biochimie
Author(s): Grégoire Rondelet, Johan Wouters
Epigenetic modifications modulate chromatin states to regulate gene expression. Among them, DNA methylation and histone modifications play a crucial role in the establishment of the epigenome. In cancer, these epigenetic events may act in concert to repress tumor suppressor genes or promote transcription of oncogenes and genes up-regulated by oncoproteins. In the context of cancer initiation and progression, recruitment of DNA (cytosine-5)-methyltransferases to specific genomic regions is mainly mediated by histone epigenetic marks, transcription factors and co-regulators as part of a dynamic process. Herein, we will review these mechanisms and present state-of-the-art of DNA methylation, treatment and development of epigenetic cancer therapies targeting this epigenetic modification.



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