DNA Methyltransferase Inhibitors: Development and Applications

  • Marie Lopez
  • Ludovic Halby
  • Paola B. ArimondoEmail author
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 945)


As described in previous chapters of this book, DNA methylation is involved in numerous biological processes, and modulation of the activity of DNA methyltransferases (DNMTs) is a powerful strategy to modulate, restore, or reduce DNA methylation. In this chapter, we will present examples of inhibitors of DNMTs (DNMTi) and review the fields of applications of DNMTi mainly as therapeutic molecules, for example, in cancers, cardiovascular or neurological diseases, but also as bioengineering tools. Finally, the limits of currently available inhibitors will be discussed and the perspectives to discover improved DNMTi will be presented.


Human Immunodeficiency Virus Methylation Level Promoter Methylation DNMT Inhibition Catalytic Pocket 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.







Alzheimer’s disease


Acute lung injury


Acute lymphoblastic leukemia


Amyotrophic lateral sclerosis


Acute myeloid leukemia




Alpha-smooth muscle actin


All-trans retinoic acid


Blood–brain barrier


Brain-derived neurotrophic factor


Bone marrow


Chronic myelomonocytic leukemia


Central nervous system




Cytosine–guanine dinucleotide


Cardiovascular disease


DNA methyltransferase


DNMT inhibitor


Endothelial cells




European Medicines Agency


Estrogen receptor


Embryonic stem cells


US Food and Drug Administration


γ-aminobutyric acid


Glutamic acid decarboxylase


Hepatitis C virus


Histone deacetylase


HDAC inhibitor


Human immunodeficiency virus


Human papilloma virus


High-throughput screening




In vitro fertilization




Long-term potentiation


Myelodysplastic syndrome


Methyl-CpG-binding protein 2


Medial prefrontal cortex


Mesenchymal stromal cells


Non-Hodgkin’s lymphomas


Neonatal maternal separation


Neuronal stem cell


Poly(ADP-ribose) polymerase


PARP inhibitor


Parkinson’s disease


Post-traumatic stress disorder




Suberoylanilide hydroxamic acid, vorinostat (Zolinza®)




Seasonal allergic rhinitis


Secreted frizzled-related protein


Secondhand smoke




Trichostatin A


Tumor suppressor gene


Valproic acid


X-ray repair cross-complementing protein


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Copyright information

© Springer International Publishing Switzerland 2016

Authors and Affiliations

  • Marie Lopez
    • 1
  • Ludovic Halby
    • 1
  • Paola B. Arimondo
    • 1
    Email author
  1. 1.CNRS FRE3600 Epigenetic Targeting of Cancer ETaC – 3Toulouse Cedex 1France

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