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bHLH-PAS proteins in cancer
David C Bersten1, Adrienne E Sullivan, Daniel J Peet
1School of Molecular and Biomedical Science (Biochemistry) and the Centre for Molecular Pathology, University of Adelaide, South Australia 5005, Australia.
Nature Reviews. Cancer
|November 23, 2013
Summary
Mammalian basic helix-loop-helix)-PER-ARNT-SIM (bHLH-PAS) proteins are crucial transcription factors. New structural insights and screening programs enable the development of targeted drugs for these important proteins.
Area of Science:
- Biochemistry and Molecular Biology
- Cellular Signaling
- Structural Biology
Background:
- Mammalian basic helix-loop-helix)-PER-ARNT-SIM (bHLH-PAS) proteins are heterodimeric transcription factors.
- These proteins respond to environmental and physiological signals via their PAS domains.
- PAS domains possess cavities for small-molecule binding and surfaces for protein interactions.
Purpose of the Study:
- To explore the structural and functional aspects of bHLH-PAS proteins.
- To identify opportunities for therapeutic intervention by targeting these proteins.
- To leverage recent structural data and screening programs for drug discovery.
Main Methods:
- Analysis of recently determined protein structures.
- Evaluation of small-molecule screening programs.
- Investigating protein-protein interactions and small-molecule binding capabilities.
Main Results:
- bHLH-PAS proteins are implicated in both pro-tumour and anti-tumour pathways.
- Their activity is modulated by natural metabolites and oncometabolites.
- Structural and screening data offer new avenues for developing selective modulators.
Conclusions:
- Structural insights into bHLH-PAS proteins are advancing drug discovery.
- Targeting bHLH-PAS proteins presents opportunities for therapeutic development.
- Selective agonists and antagonists can be developed for this versatile protein family.
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