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A concept for G protein activation by G protein-coupled receptor dimers: the transducin/rhodopsin interface

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Abstract

G protein-coupled receptors (GPCRs) are ubiquitous and essential in modulating virtually all physiological processes. These receptors share a similar structural design consisting of the seven-transmembrane α-helical segments. The active conformations of the receptors are stabilized by an agonist and couple to structurally highly conserved heterotrimeric G proteins. One of the most important unanswered questions is how GPCRs couple to their cognate G proteins. Phototransduction represents an excellent model system for understanding G protein signaling, owing to the high expression of rhodopsin in rod photoreceptors and the multidisciplinary experimental approaches used to study this GPCR. Here, we describe how a G protein (transducin) docks on to an oligomeric GPCR (rhodopsin), revealing structural details of this critical interface in the signal transduction process. This conceptual model takes into account recent structural information on the receptor and G protein, as well as oligomeric states of GPCRs.

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Authors and Affiliations

  1. International Institute of Molecular and Cell Biology, Warsaw, PL-02109, Poland

    Slawomir Filipek & Krystiana A. Krzysko

  2. Faculty of Chemistry Warsaw University, Warsaw, Poland

    Krystiana A. Krzysko

  3. M.E. Müller Institute for Microscopy Biozentrum University of Basel, CH-4056, Basel, Switzerland

    Dimitrios Fotiadis & Andreas Engel

  4. Department of Ophthalmology University of Washington, Seattle, WA, 98195, USA

    Yan Liang, David A. Saperstein & Krzysztof Palczewski

  5. Department of Pharmacology University of Washington, Seattle, WA, 98195, USA

    Krzysztof Palczewski

  6. Department of Chemistry University of Washington, Seattle, WA, 98195, USA

    Krzysztof Palczewski

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  1. Slawomir Filipek
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Filipek, S., Krzysko, K.A., Fotiadis, D. et al. A concept for G protein activation by G protein-coupled receptor dimers: the transducin/rhodopsin interface. Photochem Photobiol Sci 3, 628–638 (2004). https://doi.org/10.1039/b315661c

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