[HTML][HTML] Epidithiodiketopiperazines block the interaction between hypoxia-inducible factor-1α (HIF-1α) and p300 by a zinc ejection mechanism
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-α and the transcriptional coactivator p300.
Structure-activity studies employing both natural and synthetic ETP derivatives reveal that
only the structurally unique ETP core is required and sufficient to block the interaction of HIF …
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-α and the transcriptional coactivator p300.
Structure-activity studies employing both natural and synthetic ETP derivatives reveal that
only the structurally unique ETP core is required and sufficient to block the interaction of HIF …