Research supports HIF inhibition as a therapeutic approach for cancer 

Cancer Abnormal Cells Nucleus Genetic Division Infection Microscope

Curve Therapeutics’ CSO Ali Tavassoli has published an article in the Journal of the American Chemical Society (JACS) which highlights the potential of HIF inhibition as a therapeutic approach for cancers.

The paper is titled ‘Identification and Development of Cyclic Peptide Inhibitors of Hypoxia Inducible Factors (HIF) 1 and 2 That Disrupt Hypoxia-Related Signalling in Cancer Cells’.  

Tavassoli co-authored the article and leads the academic group at the University of Southampton where the work was undertaken. He said: “It is well recognised that HIF plays a key role in the survival and growth of solid tumours. The compounds we report in this paper inhibit the protein-protein interaction of the two subunits that form the HIF transcription factor. We show that these compounds prevent the hypoxia-induced activity of this transcription factor, stopping hypoxia-response in cell-based assays. This paper underlines the promising therapeutic potential of dual HIF inhibition as an approach for the treatment of a variety of cancers.” 

Curve is developing a non-peptidic, small-molecule dual inhibitor of HIF-1 and HIF-2 with first-in-class potential. The microcycles discovered by Professor Tavassoli were identified using his SICLOPPS screening platform and show good cellular activity.  

This is reportedly the first finding of a dual HIF-1 and HIF-2 inhibitor which functions by inhibiting the interaction of both HIF-1α and HIF-2α with HIF-1β.  

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