Keywords Demethylase, Disease, Epigenetics, Histone, Inhibitor, Lysine,
Methylation
Abbreviations
ADC
Antibody-drug conjugates
AML
Acute myelogenous leukemia
AR
Androgen receptor
ATRA
All-trans-retinoic acid
CNS
Central nervous system
DDS
Drug delivery systems
ERα
Estrogen receptor α
FAD
Flavin adenine dinucleotide
GSC
Glioma stem cells
HCF-1
Host cell factor-1
HSV
Herpes simplex virus
KDM
Lysine demethylase
KMT
Lysine methyltransferase
LSD
Lysine-specific histone demethylase
MAO
Monoamine oxidase
MDS
Myelodysplastic syndrome
NSCLC Non-small cell lung cancer
PCPA
Phenylcyclopropylamine
PDC
PCPA-drug conjugate
SCLC
Small cell lung carcinoma
siRNA
Small interfering RNA
VZV
Varicella zoster virus
1 Introduction
Histone lysine methylation is one of the epigenetic mechanisms that regulate the
expression of genes independently of the changes in DNA sequence. The methylation of histone (H) lysine (K) residues occurs at H1K26, H3K4, H3K9, H3K27,
H3K36, H3K79, and H4K20 and is responsible for transcriptional activation as well
as silencing [1, 2]. In addition, the ε-amino group of the lysine residues can undergo
mono-, di-, or trimethylation, and this differential methylation gives functional
diversity to each lysine methylation site. For example, the dimethylation of H3K4
occurs in both inactive and active genes, whereas the trimethylation is exclusive to
active genes [3]. Similarly, the monomethylation of H3K9 is seen in active genes,
whereas the trimethylation of H3K9 is associated with gene repression [4].
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T. Suzuki