Skip to main content
Journal cover image

Therapeutic potential of β-arrestin- and G protein-biased agonists.

Publication ,  Journal Article
Whalen, EJ; Rajagopal, S; Lefkowitz, RJ
Published in: Trends Mol Med
March 2011

Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor (GPCR), superfamily represent some of the most successful targets of modern drug therapy, with proven efficacy in the treatment of a broad range of human conditions and disease processes. It is now appreciated that β-arrestins, once viewed simply as negative regulators of traditional 7TMR-stimulated G protein signaling, act as multifunctional adapter proteins that regulate 7TMR desensitization and trafficking and promote distinct intracellular signals in their own right. Moreover, several 7TMR biased agonists, which selectively activate these divergent signaling pathways, have been identified. Here we highlight the diversity of G protein- and β-arrestin-mediated functions and the therapeutic potential of selective targeting of these in disease states.

Duke Scholars

Altmetric Attention Stats
Dimensions Citation Stats

Published In

Trends Mol Med

DOI

EISSN

1471-499X

Publication Date

March 2011

Volume

17

Issue

3

Start / End Page

126 / 139

Location

England

Related Subject Headings

  • beta-Arrestins
  • Signal Transduction
  • Immunology
  • Humans
  • GTP-Binding Proteins
  • Drug Therapy
  • Arrestins
  • Animals
  • 42 Health sciences
  • 32 Biomedical and clinical sciences
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Whalen, E. J., Rajagopal, S., & Lefkowitz, R. J. (2011). Therapeutic potential of β-arrestin- and G protein-biased agonists. Trends Mol Med, 17(3), 126–139. https://doi.org/10.1016/j.molmed.2010.11.004
Whalen, Erin J., Sudarshan Rajagopal, and Robert J. Lefkowitz. “Therapeutic potential of β-arrestin- and G protein-biased agonists.Trends Mol Med 17, no. 3 (March 2011): 126–39. https://doi.org/10.1016/j.molmed.2010.11.004.
Whalen EJ, Rajagopal S, Lefkowitz RJ. Therapeutic potential of β-arrestin- and G protein-biased agonists. Trends Mol Med. 2011 Mar;17(3):126–39.
Whalen, Erin J., et al. “Therapeutic potential of β-arrestin- and G protein-biased agonists.Trends Mol Med, vol. 17, no. 3, Mar. 2011, pp. 126–39. Pubmed, doi:10.1016/j.molmed.2010.11.004.
Whalen EJ, Rajagopal S, Lefkowitz RJ. Therapeutic potential of β-arrestin- and G protein-biased agonists. Trends Mol Med. 2011 Mar;17(3):126–139.
Journal cover image

Published In

Trends Mol Med

DOI

EISSN

1471-499X

Publication Date

March 2011

Volume

17

Issue

3

Start / End Page

126 / 139

Location

England

Related Subject Headings

  • beta-Arrestins
  • Signal Transduction
  • Immunology
  • Humans
  • GTP-Binding Proteins
  • Drug Therapy
  • Arrestins
  • Animals
  • 42 Health sciences
  • 32 Biomedical and clinical sciences