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Beta-arrestin-biased ligands at seven-transmembrane receptors.

Publication ,  Journal Article
Violin, JD; Lefkowitz, RJ
Published in: Trends Pharmacol Sci
August 2007

Seven-transmembrane receptors (7TMRs), the most common molecular targets of modern drug therapy, are critically regulated by beta-arrestins, which both inhibit classic G-protein signaling and initiate distinct beta-arrestin signaling. The interplay of G-protein and beta-arrestin signals largely determines the cellular consequences of 7TMR-targeted drugs. Until recently, a drug's efficacy for beta-arrestin recruitment was believed to be proportional to its efficacy for G-protein activities. This paradigm restricts 7TMR drug effects to a linear spectrum of responses, ranging from inhibition of all responses to stimulation of all responses. However, it is now clear that 'biased ligands' can selectively activate G-protein or beta-arrestin functions and thus elicit novel biological effects from even well-studied 7TMRs. Here, we discuss the current state of beta-arrestin-biased ligand research and the prospects for beta-arrestin bias as a therapeutic target. Consideration of ligand bias might have profound influences on the way scientists approach 7TMR-targeted drug discovery.

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Published In

Trends Pharmacol Sci

DOI

ISSN

0165-6147

Publication Date

August 2007

Volume

28

Issue

8

Start / End Page

416 / 422

Location

England

Related Subject Headings

  • beta-Arrestins
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Binding
  • Pharmacology & Pharmacy
  • Models, Biological
  • Ligands
  • Humans
  • Drug Design
  • Arrestins
 

Citation

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Violin, J. D., & Lefkowitz, R. J. (2007). Beta-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci, 28(8), 416–422. https://doi.org/10.1016/j.tips.2007.06.006
Violin, Jonathan D., and Robert J. Lefkowitz. “Beta-arrestin-biased ligands at seven-transmembrane receptors.Trends Pharmacol Sci 28, no. 8 (August 2007): 416–22. https://doi.org/10.1016/j.tips.2007.06.006.
Violin JD, Lefkowitz RJ. Beta-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007 Aug;28(8):416–22.
Violin, Jonathan D., and Robert J. Lefkowitz. “Beta-arrestin-biased ligands at seven-transmembrane receptors.Trends Pharmacol Sci, vol. 28, no. 8, Aug. 2007, pp. 416–22. Pubmed, doi:10.1016/j.tips.2007.06.006.
Violin JD, Lefkowitz RJ. Beta-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci. 2007 Aug;28(8):416–422.
Journal cover image

Published In

Trends Pharmacol Sci

DOI

ISSN

0165-6147

Publication Date

August 2007

Volume

28

Issue

8

Start / End Page

416 / 422

Location

England

Related Subject Headings

  • beta-Arrestins
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Binding
  • Pharmacology & Pharmacy
  • Models, Biological
  • Ligands
  • Humans
  • Drug Design
  • Arrestins