structural biology, and medicinal chemistry approaches. Our goal is to point out
herein key advances, challenges, possible future opportunities, and directions,
regarding KMT modulation in a preclinical and clinical setting.
Keywords Cancer, Chromatin, DOT1L, Epigenetic modulators, EZH2, G9a,
Lysine methyltransferases, SETs, SUVs
Abbreviations
5-HT2A
5-Hydroxytryptamine receptor 2A
AML
Acute myeloid leukemia
ASH2L
ASH2 like histone lysine methyltransferase complex
subunit
CARM1
Coactivator-associated arginine methyltransferase 1
DLBCL
Diffuse large B-cell lymphoma
DNMT
DNA methyltransferase
DNMTi
DNA methyltransferase inhibitor
DOT1L
Disruptor of telomeric silencing 1-like
EED
Embryonic ectoderm development
EHMT1
Euchromatin histone methyltransferase 1 (see also GLP)
EHMT2
Euchromatin histone methyltransferase 2 (see also G9a)
ERα
Estrogen receptor alpha
EZH1
Enhancer of zeste homologue 1
EZH2
Enhancer of zeste homologue 2
FP
Fluorescence polarization
G9a
Euchromatic
histone-lysine
N-methyltransferase
2 (EHMT2)
GLP
G9a-like protein (EHMT1)
GPCRs
G protein-coupled receptor
H1
Histamine receptor 1
H3K9
Lysine 9 of histone 3
H3K9me2
Demethylated lysine 9 of histone 3
HbF
Hemoglobin F
HCT116
Colon colorectal carcinoma cell line
HDACi
Histone deacetylase inhibitors
HEK293T
Human embryonic kidney cell line
HL60
Human leukemia cell line
HSP90
Heat shock protein 90
HTS
High-throughput screening
IUGR
Intrauterine growth restriction
KARPAS-422
Lymphoma cell line
KMTs
Lysine methyltransferases
LnCaP
Prostate adenocarcinoma cells
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