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On the histone lysine methyltransferase activity of fungal metabolite chaetocin.

Abstract:

Histone lysine methyltransferases (HKMTs) are an important class of targets for epigenetic therapy. 1 (chaetocin), an epidithiodiketopiperazine (ETP) natural product, has been reported to be a specific inhibitor of the SU(VAR)3-9 class of HKMTs. We have studied the inhibition of the HKMT G9a by 1 and functionally related analogues. Our results reveal that only the structurally unique ETP core is required for inhibition, and such inhibition is time-dependent and irreversible (in the absence of...

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Publication status:
Published

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Publisher copy:
10.1021/jm401063r

Authors


Cherblanc, FL More by this author
Chapman, KL More by this author
Sundriyal, S More by this author
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Journal:
Journal of medicinal chemistry
Volume:
56
Issue:
21
Pages:
8616-8625
Publication date:
2013-11-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:19c20c44-79eb-48ce-bb47-ce171bb48ce1
Source identifiers:
440925
Local pid:
pubs:440925

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