'7TM receptor allostery: putting numbers to shapeshifting proteins.

@article{Kenakin20097TMRA,
  title={'7TM receptor allostery: putting numbers to shapeshifting proteins.},
  author={Terry Kenakin},
  journal={Trends in pharmacological sciences},
  year={2009},
  volume={30 9},
  pages={
          460-9
        }
}
Protein allosterism is the change in protein reactivity at one site arising from a molecule binding on the protein at another site. Although allosterism traditionally has been discussed in terms of affinity changes of receptors, the increasing use of functional pharmacological assays makes it mandatory to consider effects on both the affinity and the efficacy. Antagonism of agonist response can occur allosterically by reduction of affinity and/or efficacy but the antagonist will have different… CONTINUE READING
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