Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B.

@article{Key2009PrinciplesOL,
  title={Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B.},
  author={Jason S Key and Thomas H Scheuermann and Peter C. Anderson and Valerie Daggett and Kevin H Gardner},
  journal={Journal of the American Chemical Society},
  year={2009},
  volume={131 48},
  pages={17647-54}
}
Hypoxia-inducible factors (HIFs) are heterodimeric transcription factors responsible for the metazoan hypoxia response and promote tumor growth, metastasis, and resistance to cancer treatment. The C-terminal Per-ARNT-Sim (PAS) domain of HIF2alpha (HIF2alpha PAS-B) contains a preformed solvent-inaccessible cavity that binds artificial ligands that allosterically perturb the formation of the HIF heterodimer. To better understand how small molecules bind within this domain, we examined the… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 24 extracted citations

Assembly and function of bHLH-PAS complexes.

Proceedings of the National Academy of Sciences of the United States of America • 2017

Similar Papers

Loading similar papers…