The paper outlines research conducted by Professor Ai Tavassoli, chief scientific officer at Curve, into its dual HIF-1 and HIF-2 inhibitor.
“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,” Tavassoli said.
“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.”
This publication is the first report 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.
The microcycles discovered by Tavassoli were identified using his SICLOPPS screening platform and show ‘good’ cellular activity.
Curve is focused on discovering therapies to address disease targets which are difficult to target using conventional drug discovery methods.
Through the utilisation of its Microcyle discovery platform, the company can screen directly inside mammalian cells, allowing for the identification of biologically active library members within an intracellular environment where both the library and the target are present in their native conformations.
