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Updated: May 19, 2026

Mimicking the Function of Signaling Proteins: Toward Artificial Signal Transduction Therapy
Published on: September 29, 2016
The potential for selective pharmacological therapies through biased receptor signaling
1Department 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. kenakin@email.unc.edu
Abstract:
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.
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