Screening for positive allosteric modulators: assessment of modulator concentration-response curves as a screening paradigm.

@article{Langmead2007ScreeningFP,
  title={Screening for positive allosteric modulators: assessment of modulator concentration-response curves as a screening paradigm.},
  author={Christopher James Langmead},
  journal={Journal of biomolecular screening},
  year={2007},
  volume={12 5},
  pages={668-76}
}
Targeting allosteric binding sites represents a powerful mechanism for selectively modulating receptor function. The advent of functional assays as the screening method of choice is leading to an increase in the number of allosteric modulators identified. These include positive allosteric modulators that can increase the affinity of the orthosteric agonist and potentiate the evoked response. A common method for screening for positive allosteric modulators is to examine a concentration-response… CONTINUE READING