Allosteric and Biased G Protein-Coupled Receptor Signaling Regulation: Potentials for New Therapeutics

@inproceedings{Khoury2014AllostericAB,
  title={Allosteric and Biased G Protein-Coupled Receptor Signaling Regulation: Potentials for New Therapeutics},
  author={Etienne Khoury and St{\'e}phanie Cl{\'e}ment and St{\'e}phane A Laporte},
  booktitle={Front. Endocrinol.},
  year={2014}
}
G protein-coupled receptors (GPCRs) are seven-transmembrane proteins that participate in many aspects of the endocrine function and are important targets for drug development. They transduce signals mainly, but not exclusively, via hetero-trimeric G proteins, leading to a diversity of intracellular signaling cascades. Ligands binding at the hormone orthosteric sites of receptors have been classified as agonists, antagonists, and/or inverse agonists based on their ability to mainly modulate G… CONTINUE READING

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