Analytical pharmacology and allosterism: the importance of quantifying drug parameters in drug discovery

Allosteric ligands bind to receptors at sites separate from those binding endogenous ligands; this allows for a wide range of effects from antagonism to potentiation to direct agonism. This paper discusses techniques to quantify complex allosteric behaviors that yield parameters to characterize direct effects (τB, the efficacy of allosteric agonists), α and β (the effect of the allosteric ligand on endogenous ligand affinity and efficacy respectively). These parameters are independent of the system used to determine them and thus can be used to predict allosteric effects in all systems.

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