Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.

@article{Ehlert1988EstimationOT,
  title={Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods.},
  author={Frederick J. Ehlert},
  journal={Molecular pharmacology},
  year={1988},
  volume={33 2},
  pages={
          187-94
        }
}
The theoretical basis for using radioligand binding and pharmacological techniques to estimate the dissociation constants of drugs which interact allosterically with receptors is described. This theory predicts that an allosteric ligand changes the affinity of another ligand which binds at the primary recognition site on the receptor complex without affecting the binding capacity of the primary ligand. The magnitude of this effect depends on the amount of cooperativity (positive or negative… CONTINUE READING
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