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Quantifying Biased β-Arrestin Signaling

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Arrestins - Pharmacology and Therapeutic Potential

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 219))

Abstract

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.

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Authors and Affiliations

  1. 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

    Terry Kenakin

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  1. Terry Kenakin
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Correspondence to Terry Kenakin .

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  1. Professor of Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee, USA

    Vsevolod V. Gurevich

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Kenakin, T. (2014). Quantifying Biased β-Arrestin Signaling. In: Gurevich, V. (eds) Arrestins - Pharmacology and Therapeutic Potential. Handbook of Experimental Pharmacology, vol 219. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-41199-1_3

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