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Residency time of agonists does not affect the stability of GPCR–arrestin complexes

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The interaction of arrestins with G‐protein coupled receptors (GPCRs) desensitizes agonist‐dependent receptor responses and often leads to receptor internalization. GPCRs that internalize without arrestin have been classified as “class A”… Click to show full abstract

The interaction of arrestins with G‐protein coupled receptors (GPCRs) desensitizes agonist‐dependent receptor responses and often leads to receptor internalization. GPCRs that internalize without arrestin have been classified as “class A” GPCRs whereas “class B” GPCRs co‐internalize with arrestin into endosomes. The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation. Here, we ask the question whether agonists with very slow off‐rates can cause the formation of particularly stable receptor–arrestin complexes.

Keywords: agonists affect; residency time; affect stability; arrestin; time agonists; arrestin complexes

Journal Title: British Journal of Pharmacology
Year Published: 2022

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