Abstract
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.
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Abbreviations
- 5aza:
-
5-azacytidine
- 5azadC:
-
5-aza-2′-deoxycytidine
- AD:
-
Alzheimer’s disease
- ALI:
-
Acute lung injury
- ALL:
-
Acute lymphoblastic leukemia
- ALS:
-
Amyotrophic lateral sclerosis
- AML:
-
Acute myeloid leukemia
- Ara-C:
-
Cytarabine
- ASMA:
-
Alpha-smooth muscle actin
- ATRA:
-
All-trans retinoic acid
- BBB:
-
Blood–brain barrier
- BDNF:
-
Brain-derived neurotrophic factor
- BM:
-
Bone marrow
- CMML:
-
Chronic myelomonocytic leukemia
- CNS:
-
Central nervous system
- COMT:
-
Catechol-O-methyltransferase
- CpG:
-
Cytosine–guanine dinucleotide
- CVD:
-
Cardiovascular disease
- DNMT:
-
DNA methyltransferase
- DNMTi:
-
DNMT inhibitor
- EC:
-
Endothelial cells
- EGCG:
-
(-)-epigallocatechin-3-gallate
- EMA:
-
European Medicines Agency
- ER:
-
Estrogen receptor
- ESC:
-
Embryonic stem cells
- FDA:
-
US Food and Drug Administration
- GABA:
-
γ-aminobutyric acid
- GAD:
-
Glutamic acid decarboxylase
- HCV:
-
Hepatitis C virus
- HDAC:
-
Histone deacetylase
- HDACi:
-
HDAC inhibitor
- HIV:
-
Human immunodeficiency virus
- HPV:
-
Human papilloma virus
- HTS:
-
High-throughput screening
- INFγ:
-
Interferon-γ
- IVF:
-
In vitro fertilization
- LPS:
-
Lipopolysaccharide
- LTP:
-
Long-term potentiation
- MDS:
-
Myelodysplastic syndrome
- MeCP2:
-
Methyl-CpG-binding protein 2
- mPFC:
-
Medial prefrontal cortex
- MSC:
-
Mesenchymal stromal cells
- NHL:
-
Non-Hodgkin’s lymphomas
- NMS:
-
Neonatal maternal separation
- NSC:
-
Neuronal stem cell
- PARP:
-
Poly(ADP-ribose) polymerase
- PARPi:
-
PARP inhibitor
- PD:
-
Parkinson’s disease
- PTSD:
-
Post-traumatic stress disorder
- SAH:
-
S-adenosyl-L-homocysteine
- SAHA:
-
Suberoylanilide hydroxamic acid, vorinostat (Zolinza®)
- SAM:
-
S-adenosyl-L-methionine
- SAR:
-
Seasonal allergic rhinitis
- SFRP4:
-
Secreted frizzled-related protein
- SHS:
-
Secondhand smoke
- Th:
-
T-helper
- TSA:
-
Trichostatin A
- TSG:
-
Tumor suppressor gene
- VPA:
-
Valproic acid
- XRCC1:
-
X-ray repair cross-complementing protein
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Lopez, M., Halby, L., Arimondo, P.B. (2016). DNA Methyltransferase Inhibitors: Development and Applications. In: Jeltsch, A., Jurkowska, R. (eds) DNA Methyltransferases - Role and Function. Advances in Experimental Medicine and Biology, vol 945. Springer, Cham. https://doi.org/10.1007/978-3-319-43624-1_16
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