Affordable Access

Publisher Website

Inhibitors of histone methylation

Authors
Journal
Chemico-Biological Interactions
0009-2797
Publisher
Elsevier
Publication Date
Volume
9
Issue
4
Identifiers
DOI: 10.1016/0009-2797(74)90016-7
Disciplines
  • Biology

Abstract

Abstract Two classes of inhibitors of histone methyltransferase I from calf thymus are reported. High concentrations ( ≧ 10 mM ) of various alkyl or aralkyl amines and polyamines were inhibitory to the enzyme. Spermine and spermidine were among the most potent compounds in this group. The best monoamine inhibitor was 2-phenylethylamine, which gave 47% inhibition at 10 m M. The substituted phenanthridinium compound ethidium bromide was also an inhibitor of the enzyme. A number of analogs of ethidium bromide were tested, and the most potent compound (17) gave 50% inhibition at 0.125 m M. S- Adenosyl- l- ethionine (SAM) showed competitive inhibition of the enzyme as determined from a Lineweaver-Burke plot, while ethidium bromide was noncompetitive.

There are no comments yet on this publication. Be the first to share your thoughts.

Statistics

Seen <100 times
0 Comments

More articles like this

Inhibitors of histone methylation.

on Chemico-Biological Interaction... October 1974

Histone deacetylase inhibitors decrease reelin pro...

on Journal of Neurochemistry April 2005
More articles like this..