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Epidithiodiketopiperazines block the interaction between hypoxia-inducible factor-1alpha (HIF-1alpha) and p300 by a zinc ejection mechanism.

Abstract:

The hypoxic response in humans is regulated by the hypoxia-inducible transcription factor system; inhibition of hypoxia-inducible factor (HIF) activity has potential for the treatment of cancer. Chetomin, a member of the epidithiodiketopiperazine (ETP) family of natural products, inhibits the interaction between HIF-alpha and the transcriptional coactivator p300. Structure-activity studies employing both natural and synthetic ETP derivatives reveal that only the structurally unique ETP core i...

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Publication status:
Published

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Publisher copy:
10.1074/jbc.m109.009498

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Journal:
Journal of biological chemistry More from this journal
Volume:
284
Issue:
39
Pages:
26831-26838
Publication date:
2009-09-01
DOI:
EISSN:
1083-351X
ISSN:
0021-9258

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