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Updated: Sep 12, 2025

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
Arrestins as Possible Drug Targets
Zeynep Nur Cinviz1, Elisabetta Moroni2, Ozge Sensoy1,3
1Graduate School of Engineering and Natural Sciences, Istanbul Medipol University, Istanbul 34810, Turkey.
Abstract:
Out of at least 20,000 human proteins fewer than 700 are targeted by drugs. Arrestins regulate G protein-coupled receptors, the largest family of signaling proteins in animals, as well as many receptor-independent signaling pathways. Humans express four arrestin subtypes, two of which are ubiquitous and were already shown to serve as versatile hubs of cellular signaling. So far, arrestin proteins are not directly targeted by any drugs. Here we describe potential targets on arrestins and/or interacting proteins, possible approaches for the development of targeting compounds, expected biological outcomes, and possible research and therapeutic value of targeting the interactions of arrestins with receptors and other signaling and trafficking proteins.
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