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Hypoxia inducible factor (HIF) as a model for studying inhibition of protein–protein interactions

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Abstract

The modulation of protein–protein interactions (PPIs) represents a major challenge in modern chemical biology. Current approaches (e.g. high-throughput screening, computer aided ligand design) are recognised as having limitations in terms of identification of hit matter. Considerable success has been achieved in terms of developing new approaches to PPI modulator discovery using the p53/hDM2 and Bcl-2 family of PPIs. However these important targets in oncology might be considered as “low-hanging-fruit”. Hypoxia inducible factor (HIF) is an emerging, but not yet fully validated target for cancer chemotherapy. Its role is to regulate the hypoxic response and it does so through a plethora of protein–protein interactions of varying topology, topography and complexity: its modulation represents an attractive approach to prevent development of new vasculature by hypoxic tumours.

Graphical abstract: Hypoxia inducible factor (HIF) as a model for studying inhibition of protein–protein interactions

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Publication details

The article was received on 25 Jan 2017, accepted on 31 Mar 2017 and first published on 26 Apr 2017


Article type: Perspective
DOI: 10.1039/C7SC00388A
Citation: Chem. Sci., 2017, Advance Article
  • Open access: Creative Commons BY license
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    Hypoxia inducible factor (HIF) as a model for studying inhibition of protein–protein interactions

    G. M. Burslem, H. F. Kyle, A. Nelson, T. A. Edwards and A. J. Wilson, Chem. Sci., 2017, Advance Article , DOI: 10.1039/C7SC00388A

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