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The arrestin-receptor complex: Exciting answers and new questions

The Structural Basis of Arrestin Functions, Page: 175-184
2017
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Book Chapter Description

To better understand the molecular mechanism of arrestin-mediated signaling, detailed structural information on the arrestin-receptor complex is necessary. Biochemical studies provided some information about how arrestins are recruited by active receptors. The X-ray laser crystal structure of the rhodopsinarrestin complex reveals unique structural features, which include the asymmetric binding of arrestin to rhodopsin. Arrestin adopts the active conformation, with a ~20° rotation between the N- and C-domains of the molecule, which opens up a cleft in arrestin to accommodate a short helix formed by the second intracellular loop of rhodopsin. Rhodopsin-arrestin complex gives important insights into how G protein-coupled receptor signaling is terminated by arrestin and reveals structural basis of the mechanism of arrestin-biased signaling.

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