Journal
TRENDS IN MOLECULAR MEDICINE
Volume 17, Issue 3, Pages 126-139Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.molmed.2010.11.004
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Funding
- Howard Hughes Medical Institute Funding Source: Medline
- NHLBI NIH HHS [R01 HL070631, R01 HL016037] Funding Source: Medline
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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 beta-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 beta-arrestin-mediated functions and the therapeutic potential of selective targeting of these in disease states.
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