Biased G Protein-Coupled Receptor Signaling: New Player in Modulating Physiology and Pathology
Biomolecules & Therapeutics
;
: 12-25, 2017.
Article
in English
| WPRIM
| ID: wpr-165941
ABSTRACT
G protein-coupled receptors (GPCRs) are a family of cell-surface proteins that play critical roles in regulating a variety of pathophysiological processes and thus are targeted by almost a third of currently available therapeutics. It was originally thought that GPCRs convert extracellular stimuli into intracellular signals through activating G proteins, whereas β-arrestins have important roles in internalization and desensitization of the receptor. Over the past decade, several novel functional aspects of β-arrestins in regulating GPCR signaling have been discovered. These previously unanticipated roles of β-arrestins to act as signal transducers and mediators of G protein-independent signaling have led to the concept of biased agonism. Biased GPCR ligands are able to engage with their target receptors in a manner that preferentially activates only G protein- or β-arrestin-mediated downstream signaling. This offers the potential for next generation drugs with high selectivity to therapeutically relevant GPCR signaling pathways. In this review, we provide a summary of the recent studies highlighting G protein- or β-arrestin-biased GPCR signaling and the effects of biased ligands on disease pathogenesis and regulation.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Physiology
/
Transducers
/
Bias
/
Felodipine
/
GTP-Binding Proteins
/
Ligands
Limits:
Humans
Language:
English
Journal:
Biomolecules & Therapeutics
Year:
2017
Type:
Article
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