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PMID: 21183406 Published · ppublish English Journal Article Review

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

Trends in molecular medicine ·Vol. 17 ·No. 3 ·2011-03-00 ·Pages 126-39

Whalen EJ, Rajagopal S, Lefkowitz RJ

Abstract

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.

MeSH Terms
Animals Arrestins/agonists,therapeutic use Drug Therapy GTP-Binding Proteins/agonists,therapeutic use Humans Signal Transduction beta-Arrestins
Chemicals
Arrestins beta-Arrestins GTP-Binding Proteins
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Whalen Erin J
Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA.
Rajagopal Sudarshan
Lefkowitz Robert J
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Article Info
Journal
Trends in molecular medicine
Abbr.
Trends Mol Med
ISSN
1471-499X
DOI
10.1016/j.molmed.2010.11.004
Published
2011-03-00
Epub
2010-00-21
Pages
126-39
Language
English
Region
England
NLM ID
100966035
PMCID
PMC3628754
Subset
IM
Grants
Howard Hughes Medical Institute · United States
NHLBI NIH HHS · R01 HL016037 · United States
NHLBI NIH HHS · R01 HL070631 · United States
External Links
PubMed source DOI: 10.1016/j.molmed.2010.11.004 PMC Full Text View journal details
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