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Synthesis and biological evaluation of tripartin, a putative KDM4 natural product inhibitor, and 1‐Dichloromethylinden‐1‐ol analogues

Abstract:

The natural product tripartin has been reported to inhibit the N‐methyl‐lysine histone demethylase KDM4A. A synthesis of tripartin starting from 3,5‐dimethoxyphenylacrylic acid was developed, and the enantiomers were separated by chiral HPLC. We observed that both tripartin enantiomers manifested an apparent increase in H3K9me3 levels when dosed in cells, as measured by western blot analysis. Thus, there is no enantiomeric discrimination toward this natural product in terms of its effects on ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1002/cmdc.201800377

Authors


Guillade, L More by this author
Tarhonskaya, H More by this author
Nebbioso, A More by this author
Alvarez, S More by this author
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Cost Action CM-1406 More from this funder
Wellcome Trust More from this funder
Cancer Research UK More from this funder
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Publisher:
John Wiley and Sons, Ltd. Publisher's website
Journal:
ChemMedChem Journal website
Volume:
13
Issue:
18
Pages:
1949-1956
Publication date:
2018-07-26
Acceptance date:
2018-07-01
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
Pubs id:
pubs:909545
URN:
uri:4dc7303f-51e1-452e-a5f0-138ac4ad4f39
UUID:
uuid:4dc7303f-51e1-452e-a5f0-138ac4ad4f39
Local pid:
pubs:909545

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