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CREB binding protein (CREBBP; CBP); E1A binding protein p300 (EP300; p300); hypoxia-inducible
factor 1a
(HIF1A; HIF1a)

In vitro and mouse studies suggest peptide inhibitors of HIF1A could help treat cancer. In human breast cancer cells, two stabilized peptide helix mimetics that block the interaction between HIF1A and its coactivators CBP or p300 decreased hypoxia-inducible transcription of target genes including VEGF-A compared with vehicle. In mouse xenograft models of human renal cell carcinoma, one of the mimetics decreased tumor volume compared with no treatment. Next steps could include testing the peptide mimetic in additional animal models.
At least seven companies have HIF1A inhibitors in Phase II or earlier testing to treat various cancers.

SciBX 6(39); doi:10.1038/scibx.2013.1088
Published online Oct. 10, 2013

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Kushal, S. et al. Proc. Natl. Acad. Sci. USA; published online Sept. 9, 2013;
Contact: Paramjit S. Arora, New York University, New York, N.Y.
Contact: Bogdan Z. Olenyuk, University of Southern California,
Los Angeles, Calif.