Abstract
Interleukin-1 (IL-1) induces the internalization of its cognate receptor from the plasma membrane. However, it has remained elusive as to how this mechanism affects the IL-1-induced signal transduction. In this study, we used small-molecule inhibitors of receptor endocytosis to analyze the effects on IL-1-induced signal transduction pathways. We demonstrate that the inhibition of endocytosis down-modulates IL-1-induced NF-κB-dependent gene expression at a level downstream of nuclear translocation and DNA binding of NF-κB. Moreover, we report that the reduced NF-κB-dependent gene expression disrupts feedback inhibition loops terminating the activation of mitogen-activated protein kinases and down-regulating the expression of IL-1-induced mRNAs. Collectively, we show that the inhibition of endocytosis causes a dysregulation of IL-1-induced signal transduction and gene expression demonstrating an important role for receptor internalization in IL-1 signaling.
Copyright © 2012 Elsevier Inc. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cell Line
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DNA / metabolism
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Down-Regulation / drug effects
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Dynamins / antagonists & inhibitors
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Dynamins / metabolism
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Endocytosis / drug effects*
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HEK293 Cells
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Humans
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Hydrazones / pharmacology
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I-kappa B Proteins / genetics
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I-kappa B Proteins / metabolism
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Interleukin-1 / genetics
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Interleukin-1 / metabolism
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Interleukin-1 / pharmacology*
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Interleukin-8 / genetics
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Interleukin-8 / metabolism
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Ligands
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Mice
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Mitogen-Activated Protein Kinases / genetics
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Mitogen-Activated Protein Kinases / metabolism
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NF-KappaB Inhibitor alpha
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NF-kappa B / genetics
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NF-kappa B / metabolism*
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Receptors, Interleukin-1 / antagonists & inhibitors
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Receptors, Interleukin-1 / metabolism*
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Recombinant Proteins / biosynthesis
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Recombinant Proteins / genetics
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Recombinant Proteins / pharmacology
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Signal Transduction / drug effects
Substances
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Hydrazones
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I-kappa B Proteins
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Interleukin-1
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Interleukin-8
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Ligands
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N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthahydrazide
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NF-kappa B
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NFKBIA protein, human
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Nfkbia protein, mouse
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Receptors, Interleukin-1
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Recombinant Proteins
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NF-KappaB Inhibitor alpha
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DNA
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Mitogen-Activated Protein Kinases
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Dynamins