Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes.

@article{Smith2010AllosteryAG,
  title={Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes.},
  author={Nicola J Smith and Graeme Milligan},
  journal={Pharmacological reviews},
  year={2010},
  volume={62 4},
  pages={701-25}
}
For many years seven transmembrane domain G protein-coupled receptors (GPCRs) were thought to exist and function exclusively as monomeric units. However, evidence both from native cells and heterologous expression systems has demonstrated that GPCRs can both traffic and signal within higher-order complexes. As for other protein-protein interactions, conformational changes in one polypeptide, including those resulting from binding of pharmacological ligands, have the capacity to alter the… CONTINUE READING