Targeting DNA methylation for epigenetic therapy

X Yang, F Lay, H Han, PA Jones - Trends in pharmacological sciences, 2010 - cell.com
… further efforts to elucidate epigenetic alterations in cancer, and to subsequently develop new
epigenetic therapies. This review delineates the latest cancer epigenetic models, the recent …

DNA methyltransferase inhibitors in cancer: from pharmacology to translational studies

D Pechalrieu, C Etievant, PB Arimondo - Biochemical pharmacology, 2017 - Elsevier
… to extend our understanding of DNA methylation and its implication in several diseases. The
… field for DNMT inhibition. However, efficient and potent targeting of DNA methylation in cells …

[HTML][HTML] The promise for histone methyltransferase inhibitors for epigenetic therapy in clinical oncology: a narrative review

HS Rugo, I Jacobs, S Sharma, F Scappaticci… - … in therapy, 2020 - Springer
… (DNMTs) to specific genomic loci to promote DNA methylation [19,20,21]. On the … DNA
methylation and histone modification machinery critical for maintaining the cellular epigenetic

Epigenetic drug discovery: targeting DNA methyltransferases

JM Foulks, KM Parnell, RN Nix… - Journal of …, 2012 - journals.sagepub.com
role of human DNA methyltransferases (DNMTs) in cancer as well as the therapeutic potential
and challenge of inhibitingEpigenetic therapy may reverse either silenced or repressed …

[HTML][HTML] Biological rationale for the use of DNA methyltransferase inhibitors as new strategy for modulation of tumor response to chemotherapy and radiation

GL Gravina, C Festuccia, F Marampon, VM Popov… - Molecular cancer, 2010 - Springer
DNA methyltransferase (DNMT) inhibitors represent a promising class of … , DNA methylation
is one of the most extensively characterized epigenetic modifications and its biological role is …

[HTML][HTML] DNA methyltransferase inhibitors—state of the art

J Goffin, E Eisenhauer - Annals of Oncology, 2002 - Elsevier
… , and it offers a target for the treatment of malignancy [2, 3]. In this review, methylation, its
role in cancer and the therapeutic agents that affect methylation will be described. …

The role of epigenetic transcription repression and DNA methyltransferases in cancer

FI Daniel, K Cherubini, LS Yurgel, MAZ de Figueiredo… - Cancer, 2011 - Wiley Online Library
… This review summarizes the main epigenetic mechanisms involved in cancer development,
with special focus on DNA methyltransferase enzymes and hypermethylation of tumor

Emerging epigenetic targets and therapies in cancer medicine

R Popovic, JD Licht - Cancer discovery, 2012 - AACR
… We review emerging epigenetic targets in cancer and present recent models of … epigenetic
therapies. Significance: The use of DNA methyltransferase and histone deacetylase inhibitors

[HTML][HTML] Expanding the structural diversity of DNA methyltransferase inhibitors

KE Juárez-Mercado, FD Prieto-Martínez… - Pharmaceuticals, 2020 - mdpi.com
… scaffolds, herein, we report five new inhibitors of DNMT1 with distinct chemical scaffolds. Two
inhibitor (HDAC), another major epigenetic target, and could be used as a dual epigenetic

[HTML][HTML] Advances in epigenetic cancer therapeutics

C Hillyar, KS Rallis, J Varghese - Cureus, 2020 - ncbi.nlm.nih.gov
Epigenetic modifications, including DNA methylation and demethylation and histone …
Hence, epigenetic therapy has emerged as a rapidly advancing field of cancer research. A …