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2017 ; 36
(13
): 1753-1759
Nephropedia Template TP
gab.com Text
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English Wikipedia
Epigenetic therapies by targeting aberrant histone methylome in AML: molecular
mechanisms, current preclinical and clinical development
#MMPMID27593928
Tsai CT
; So CW
Oncogene
2017[Mar]; 36
(13
): 1753-1759
PMID27593928
show ga
While the current epigenetic drug development is still largely restricted to
target DNA methylome, emerging evidence indicates that histone methylome is
indeed another major epigenetic determinant for gene expression and frequently
deregulated in acute myeloid leukaemia (AML). The recent advances in dissecting
the molecular regulation and targeting histone methylome in AML together with the
success in developing lead compounds specific to key histone
methylation-modifying enzymes have revealed new opportunities for effective
leukaemia treatment. In this article, we will review the emerging functions of
histone methyltransferases and histone demethylases in AML, especially
MLL-rearranged leukaemia. We will also examine recent preclinical and clinical
studies that show significant promises of targeting these histone
methylation-modifying enzymes for AML treatment.
|Acetylation
[MESH]
|Animals
[MESH]
|Antineoplastic Agents/*pharmacology/therapeutic use
[MESH]