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Quantifying Biased β-Arrestin Signaling.
MedLine Citation:
PMID:  24292824     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
It is now established that agonists do not uniformly activate pleiotropic signaling mechanisms initiated by receptors but rather can bias signals according to the unique receptor conformations they stabilize. One of the important emerging signaling systems where this can occur is through β-arrestin. This chapter discusses biased signaling where emphasis or de-emphasis of β-arrestin signaling is postulated (or been shown) to be beneficial. The chapter specifically focuses on methods to quantify biased effects; these methods furnish scales that can be used in the process of optimizing biased agonism (and antagonism) for therapeutic benefit. Specifically, methods to derive ΔΔLog(τ/K A) or ΔΔLog(Relative Activity) values are described to do this.
Authors:
Terry Kenakin
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Handbook of experimental pharmacology     Volume:  219     ISSN:  0171-2004     ISO Abbreviation:  Handb Exp Pharmacol     Publication Date:  2014  
Date Detail:
Created Date:  2013-12-02     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7902231     Medline TA:  Handb Exp Pharmacol     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  57-83     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, University of North Carolina School of Medicine, 120 Mason Farm Road, Room 4042, Genetic Medicine Building, CB# 7365, Chapel Hill, NC, 27599-7365, USA, Kenakin@email.unc.edu.
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