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Development of novel bisubstrate-type inhibitors of histone methyltransferase SET7/9.

Abstract：

:Histone modification, for example, by histone deacetylase (HDAC) and histone lysine methyltransferase (HMT), plays an important role in regulating gene expression. To obtain novel inhibitors as tools for investigating the physiological function of members of the HMT family, we designed and synthesized novel inhibitors, which are amine analogues of adenosylmethionine (AdoMet; the cofactor utilized in the methylation reaction) bearing various alkylamino groups coupled via an ethylene linker. The inhibitory activities of these compounds towards SET7/9, an HMT, were evaluated. It was found that introduction of an alkylamino group increased the inhibitory activity.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Mori S,Iwase K,Iwanami N,Tanaka Y,Kagechika H,Hirano T

doi

10.1016/j.bmc.2010.10.022

subject

Has Abstract

pub_date

2010-12-01 00:00:00

pages

8158-66

issue

23

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00945-4

journal_volume

18

pub_type

杂志文章

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