Modulation of the hypoxic response in cancer; inhibition of the HIF-1α/p300 protein-protein interaction
Hypoxia inducible factor (HIF)-1α is a heterodimerically-activated transcription factor central to the cellular response to hypoxic environments and is often upregulated in cancer. Binding of HIF-1α to the co-activator p300 is necessary for the hypoxia-induced transcription of many oncogenic proteins. The aim of this project was to develop novel small molecule inhibitors of the HIF-1α/p300 protein-protein interaction (PPI).
Initial work focused on designing, validating and optimisin...Expand abstract
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- Oxford University, UK
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- Jayatunga, M
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