Targeting DNA methylation for epigenetic therapy

X Yang, F Lay, H Han, PA Jones - Trends in pharmacological sciences, 2010 - cell.com
Patterns of DNA methylation are established during embryonic development and faithfully
copied through somatic cell divisions. Based on current understanding of DNA methylation …

DNA methylation as a therapeutic target in cancer

JPJ Issa - Clinical Cancer Research, 2007 - AACR
Targeting DNA methylation for cancer therapy has had a rocky history. The first reports on
DNA methylation changes in cancer described global loss of methylation, which has been …

Digging deep into “dirty” drugs–modulation of the methylation machinery

L Pleyer, R Greil - Drug metabolism reviews, 2015 - Taylor & Francis
DNA methylation and histone modification are epigenetic mechanisms that result in altered
gene expression and cellular phenotype. The exact role of methylation in myelodysplastic …

Targeting DNA methylation

JPJ Issa, HM Kantarjian - Clinical Cancer Research, 2009 - AACR
Two nucleoside inhibitors of DNA methylation, azacitidine and decitabine, are now standard
of care for the treatment of the myelodysplastic syndrome, a deadly form of leukemia. These …

Reactivation of epigenetically silenced genes by DNA methyltransferase inhibitors: basic concepts and clinical applications

C Mund, B Brueckner, F Lyko - Epigenetics, 2006 - Taylor & Francis
Hypermethylation of tumor suppressor genes is one of the most consistent hallmarks of
human cancers. This epigenetic alteration has been associated with gene silencing and …

DNA hypomethylating drugs in cancer therapy

T Sato, JPJ Issa, P Kropf - Cold Spring …, 2017 - perspectivesinmedicine.cshlp.org
Aberrant DNA methylation is a critically important modification in cancer cells, which,
through promoter and enhancer DNA methylation changes, use this mechanism to activate …

DNA methylation and gene silencing in cancer

SB Baylin - Nature clinical practice Oncology, 2005 - nature.com
Epigenetic changes such as DNA methylation act to regulate gene expression in normal
mammalian development. However, promoter hypermethylation also plays a major role in …

DNA methyltransferase inhibitors in cancer: from pharmacology to translational studies

D Pechalrieu, C Etievant, PB Arimondo - Biochemical pharmacology, 2017 - Elsevier
DNA methylation is a mammalian epigenetic mark that participates to define where and
when genes are expressed, both in normal cells and in the context of diseases. Like other …

[HTML][HTML] Clinical development of demethylating agents in hematology

SC Navada, J Steinmann, M Lübbert… - The Journal of …, 2014 - Am Soc Clin Investig
The term epigenetics refers to the heritable changes in gene expression that are not
associated with a change in the actual DNA sequence. Epigenetic dysregulation is linked to …

The DNA methylation landscape of hematological malignancies: an update

P Blecua, L Martinez‐Verbo, M Esteller - Molecular Oncology, 2020 - Wiley Online Library
The rapid advances in high‐throughput sequencing technologies have made it more evident
that epigenetic modifications orchestrate a plethora of complex biological processes. During …