Allosteric targeting of receptor tyrosine kinases

  title={Allosteric targeting of receptor tyrosine kinases},
  author={Frederik De Smet and Arthur Christopoulos and Peter Carmeliet},
  journal={Nature Biotechnology},
The drug discovery landscape has been transformed over the past decade by the discovery of allosteric modulators of all major mammalian receptor superfamilies. Allosteric ligands are a rich potential source of drugs and drug targets with clear therapeutic advantages. G protein–coupled receptors, ligand-gated ion channels and intracellular nuclear hormone receptors have all been targeted by allosteric modulators. More recently, a receptor tyrosine kinase (RTK) has been targeted by an… 
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Nuclear hormone receptors: Allosteric switches
  • I. McEwan
  • Biology
    Molecular and Cellular Endocrinology
  • 2012
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The studies thus far have been performed with the estrogen receptors, the androgen receptor (AR), the thyroid hormone receptors, and the pregnane X receptor, and identified small molecule modulators that are believed to function through the NRs but have, as yet, unknown sites and mechanisms of action.