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Review
. 2018 May 29;137(22):2315-2317.
doi: 10.1161/CIRCULATIONAHA.117.028194.

Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery

James W Wisler  1 , Howard A Rockman  1   2   3 , Robert J Lefkowitz  4   5   6
Affiliations
Review

Biased G Protein-Coupled Receptor Signaling: Changing the Paradigm of Drug Discovery

James W Wisler et al. Circulation. .
No abstract available

Keywords: GTP-binding proteins; cardiovascular agents; heart failure; ligands; receptor, angiotensin, type 1; receptors, adrenergic.

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Conflict of interest statement

Conflict of Interest Disclosures: RJL and HAR report they are scientific co-founders and stockholders of Trevena, Inc. JWW has no potential conflicts to disclose.

Figures

Figure 1
Figure 1. Potential pharmacologic mechanisms of biased G protein-coupled receptor signaling
Multiple potential classes of biased pharmacologic compounds targeting GPCRs have been identified. These range from orthosteric ligands that interact with the binding site of the endogenous ligand, to allosteric modulators that bind a receptor at a site distinct from the endogenous ligand, to bitopic ligands that bind at both orthosteric and allosteric sites.
See this image and copyright information in PMC

References

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