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The potential for selective pharmacological therapies through biased receptor signaling

Terry Kenakin

Author affiliations

Department of Pharmacology, University of North Carolina School of Medicine, 120 Mason Farm Road, Room 4042 Genetic Medicine Building, CB# 7365, Chapel Hill, NC, 27599-7365, USA

Citation and License

BMC Pharmacology and Toxicology 2012, 13:3  doi:10.1186/2050-6511-13-3

Published: 13 August 2012


The discovery that not all agonists uniformly activate cellular signaling pathways (biased signaling) has greatly changed the drug discovery process for agonists and the strategy for treatment of disease with agonists. Technological advances have enabled complex receptor behaviors to be viewed independently and through these assays, the bias for an agonist can be quantified. It is predicted that therapeutic phenotypes will be linked, through translational studies, to quantified scales of bias to guide medicinal chemists in the drug discovery process.