Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands.

@article{Avlani2007CriticalRF,
  title={Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands.},
  author={Vimesh A. Avlani and Karen J Gregory and Craig J Morton and Michael W. Parker and Patrick M. Sexton and Arthur Christopoulos},
  journal={The Journal of biological chemistry},
  year={2007},
  volume={282 35},
  pages={
          25677-86
        }
}
  • Vimesh A. Avlani, Karen J Gregory, +3 authors Arthur Christopoulos
  • Published in
    The Journal of biological…
    2007
  • Chemistry, Medicine
  • The second extracellular (E2) loop of G protein-coupled receptors (GPCRs) plays an essential but poorly understood role in the binding of non-peptidic small molecules. We have utilized both orthosteric ligands and allosteric modulators of the M2 muscarinic acetylcholine receptor, a prototypical Family A GPCR, to probe possible E2 loop binding dynamics. We developed a homology model based on the crystal structure of bovine rhodopsin and predicted novel cysteine substitutions that should… CONTINUE READING

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