Efficacy at g-protein-coupled receptors

@article{Kenakin2002EfficacyAG,
  title={Efficacy at g-protein-coupled receptors},
  author={Terry Kenakin},
  journal={Nature Reviews Drug Discovery},
  year={2002},
  volume={1},
  pages={103-110}
}
At present, the drug-discovery process centres on ligands that either block or produce physiological responses. However, there are therapeutic uses for ligands that do neither of these things, but which still affect receptors in other ways. This review discusses the intimate relationship between the affinity of a ligand for its receptor, and the probability that the binding of the ligand will produce some change in the receptor, resulting in efficacy. This, in turn, argues that ligands that… CONTINUE READING

From This Paper

Figures, tables, and topics from this paper.

Explore Further: Topics Discussed in This Paper

Citations

Publications citing this paper.
Showing 1-10 of 93 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 91 references

Drug efficacy at G protein-coupled receptors.

Annual review of pharmacology and toxicology • 2002

Can allosteric regulation be predicted from structure?

Proceedings of the National Academy of Sciences of the United States of America • 2000

The Pharmacology of Functional, Biochemical, and Recombinant Systems

H. O. Onaran, A. Scheer, S. Cotecchia, T. Costa
Handbook of Experimental Pharmacology • 2000

Constitutive receptor systems for drug discovery.

Journal of pharmacological and toxicological methods • 1999

Similar Papers

Loading similar papers…