Endogenous allosteric modulators of G protein-coupled receptors.

  title={Endogenous allosteric modulators of G protein-coupled receptors.},
  author={Emma T van der Westhuizen and C{\'e}line Valant and Patrick M. Sexton and Arthur Christopoulos},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={353 2},
G protein-coupled receptors (GPCRs) are the largest superfamily of receptors encoded by the human genome, and represent the largest class of current drug targets. Over the last decade and a half, it has become widely accepted that most, if not all, GPCRs possess spatially distinct allosteric sites that can be targeted by exogenous substances to modulate the receptors' biologic state. Although many of these allosteric sites are likely to serve other (e.g., structural) roles, they nonetheless… CONTINUE READING
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