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Molecular determinants on extracellular loop domains that dictate interaction between β-arrestin and human APJ receptor
Published in Wiley Blackwell
2019
PMID: 30801688
Volume: 593
   
Issue: 6
Pages: 634 - 643
Abstract
The human APJ receptor (APJR), activated by apelin isoforms, regulates cardiovascular functions and fluid homeostasis. Understanding its structure-function relationship is crucial for a comprehensive knowledge of signalling aberrations that cause several physiological disorders. Here, we demonstrate the influence of extracellular loop (ECL) domains in the mechanism of β-arrestin-mediated signalling from human APJR: Apelin system. Alanine mutations of evolutionarily conserved residues were characterized using receptor internalization, β-arrestin pull-down, Akt phosphorylation and cell migration assay. C281A and 268KTL270-AAA in ECL3 were deficient in all assays, whereas 183MDYS186-AAAA mutant in ECL2 showed impaired β-arrestin-mediated signalling but demonstrated Gi-dependent cell migration. Our findings establish that conserved residues in the extracellular domain play a prominent role in modulating receptor interactions with the β-arrestin signalling cascade. © 2019 Federation of European Biochemical Societies
About the journal
JournalData powered by TypesetFEBS Letters
PublisherData powered by TypesetWiley Blackwell
ISSN00145793
Open AccessNo
Concepts (29)
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    ADENINE
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    Alanine
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    APELIN
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    APELIN RECEPTOR
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    Aspartic acid
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    BETA ARRESTIN
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    Cytosine
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    Leucine
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    Lysine
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    Methionine
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    Protein kinase b
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    Serine
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    Threonine
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    Tyrosine
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    Article
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    Cell migration
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    Extracellular space
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    Genetic conservation
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    Human
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    Human cell
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    Molecular mechanics
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    Mutational analysis
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    Nonhuman
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    Priority journal
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    Protein domain
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    Protein phosphorylation
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    Protein protein interaction
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    Receptor binding
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    Signal transduction