Tripartin, a Histone Demethylase Inhibitor from a Bacterium Associated with a Dung Beetle Larva

Tripartin (1), a new dichlorinated indanone, was isolated from the culture broth of the Streptomyces sp. associated with a larva of the dung beetle Copris tripartitus Waterhouse. The planar structure of tripartin (1) was identified by the spectroscopic analyses of NMR, mass, UV, and IR data. The str...

Full description

Saved in:
Bibliographic Details
Published in:Organic letters 2013-04, Vol.15 (8), p.1834-1837
Main Authors: Kim, Seong-Hwan, Kwon, So Hee, Park, Seon-Hui, Lee, Jae Kyun, Bang, Hea-Son, Nam, Sang-Jip, Kwon, Hak Cheol, Shin, Jongheon, Oh, Dong-Chan
Format: Article
Language:English
Subjects:
Animals
Coleoptera - microbiology
Crystallography, X-Ray
HeLa Cells
Histone Demethylases - antagonists & inhibitors
Humans
Hydrocarbons, Chlorinated - chemistry
Hydrocarbons, Chlorinated - isolation & purification
Hydrocarbons, Chlorinated - pharmacology
Indans - chemistry
Indans - isolation & purification
Indans - pharmacology
Larva - microbiology
Molecular Structure
Nuclear Magnetic Resonance, Biomolecular
Streptomyces - chemistry
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Tripartin (1), a new dichlorinated indanone, was isolated from the culture broth of the Streptomyces sp. associated with a larva of the dung beetle Copris tripartitus Waterhouse. The planar structure of tripartin (1) was identified by the spectroscopic analyses of NMR, mass, UV, and IR data. The structure was confirmed, and the absolute configuration of 1 was determined by X-ray crystallography. Tripartin displayed specific activity as an inhibitor of the histone H3 lysine 9 demethylase KDM4 in HeLa cells.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol4004417