Euchromatic histone methyltransferase 2 inhibitor, BIX-01294, sensitizes human promyelocytic leukemia HL-60 and NB4 cells to growth inhibition and differentiation.

Abstract:

:The involvement of histone lysine methyltransferases (HMT) in carcinogenesis is not well understood. Here, we describe a dose-dependent growth and survival inhibitory effects of BIX-01294, a specific inhibitor of euchromatic HMT2, in promyelocytic leukemia HL-60 and NB4 cells. BIX-01294 combined with all-trans retinoic acid or together with histone deacetylase and DNA methyltransferase inhibitors enhanced cell differentiation to granulocytes and induced cell line-specific changes in the expression of cell cycle-, survival- and differentiation regulating genes and proteins in association with histone modification state. Our results suggest that targeting EHMT2 may be of therapeutical benefits in myeloid leukemia.

journal_name

Leuk Res

journal_title

Leukemia research

authors

Savickiene J,Treigyte G,Stirblyte I,Valiuliene G,Navakauskiene R

doi

10.1016/j.leukres.2014.04.003

subject

Has Abstract

pub_date

2014-07-01 00:00:00

pages

822-9

issue

7

eissn

0145-2126

issn

1873-5835

pii

S0145-2126(14)00114-3

journal_volume

38

pub_type

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