G Protein-coupled Receptor Biased Agonism.
Publication/Presentation Date
3-1-2016
Abstract
G protein-coupled receptors are the largest family of targets for current therapeutics. The classic model of their activation was binary, where agonist binding induced an active conformation and subsequent downstream signaling. Subsequently, the revised concept of biased agonism emerged, where different ligands at the same G protein-coupled receptor selectively activate one downstream pathway versus another. Advances in understanding the mechanism of biased agonism have led to the development of novel ligands, which have the potential for improved therapeutic and safety profiles. In this review, we summarize the theory and most recent breakthroughs in understanding biased signaling, examine recent laboratory investigations concerning biased ligands across different organ systems, and discuss the promising clinical applications of biased agonism.
Volume
67
Issue
3
First Page
193
Last Page
202
ISSN
1533-4023
Published In/Presented At
Hodavance, S. Y., Gareri, C., Torok, R. D., & Rockman, H. A. (2016). G Protein-coupled Receptor Biased Agonism. Journal of cardiovascular pharmacology, 67(3), 193–202. https://doi.org/10.1097/FJC.0000000000000356
Disciplines
Medicine and Health Sciences
PubMedID
26751266
Department(s)
Department of Medicine, Cardiology Division
Document Type
Article