Abstract
Tyrosine kinase cascades may play a role in the hypoxic regulation of hypoxia-inducible factor (HIF)-1. We investigated the role of tyrosine kinase phosphorylation and of the Shc/Ras cascade on hypoxic HIF-1 stabilization. Exposure of human umbilical vein endothelial cells to hypoxia results in HIF protein stabilization as early as 10 minutes, with a maximum at 3 hours, and also in Shc tyrosine phosphorylation, with a maximum at 10 minutes. To test whether Shc directly mediates hypoxia-induced HIF stabilization, human umbilical vein endothelial cells were transfected with a dominant-negative Shc mutant (dnShc), resulting in significantly reduced HIF protein levels compared with control. Similar results were obtained with cells transfected with dominant-negative Ras, a known downstream effector of Shc. Hypoxia-induced Ras activity was significantly reduced in cells transfected with dnShc compared with control levels, indicating that Ras indeed acts downstream from Shc. Moreover, cells pretreated with a specific Raf-1 kinase inhibitor, a known downstream effector of Ras, exhibited reduced HIF protein levels. To examine the functional consequences of Shc in hypoxic signaling, HIF-1 ubiquitination, protein stabilization, and endothelial cell migration were assessed. Overexpression of dnShc increased ubiquitination of HIF-1 and reduced the half-life of the protein. Moreover, dnShc, dominant-negative Ras, or the Raf-1 kinase inhibitor significantly inhibited migration under hypoxia. Thus, Shc in concert with Ras and Raf-1 contributes to hypoxia-induced HIF-1alpha protein stabilization and endothelial cell migration.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adaptor Proteins, Signal Transducing*
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Adaptor Proteins, Vesicular Transport*
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Blotting, Western
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Cell Hypoxia / physiology
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Cell Line
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Cell Movement / drug effects
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Cobalt / pharmacology
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Cycloheximide / pharmacology
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DNA-Binding Proteins / metabolism*
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Endothelium, Vascular / cytology
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Endothelium, Vascular / drug effects
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Endothelium, Vascular / metabolism*
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Enzyme Inhibitors / pharmacology
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Humans
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Hypoxia-Inducible Factor 1
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Hypoxia-Inducible Factor 1, alpha Subunit
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Mutation
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Nuclear Proteins / metabolism*
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Plasmids / genetics
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Proteins / genetics
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Proteins / metabolism*
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Proto-Oncogene Proteins c-raf / antagonists & inhibitors
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Proto-Oncogene Proteins c-raf / metabolism
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Pyrazoles / pharmacology
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Pyrimidines / pharmacology
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Shc Signaling Adaptor Proteins
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Src Homology 2 Domain-Containing, Transforming Protein 1
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Transcription Factors*
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Transfection
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Tyrphostins / pharmacology
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Ubiquitin / metabolism
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ras Proteins / genetics
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ras Proteins / metabolism
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src-Family Kinases / antagonists & inhibitors
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src-Family Kinases / metabolism
Substances
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4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo(3,4-d)pyrimidine
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Adaptor Proteins, Signal Transducing
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Adaptor Proteins, Vesicular Transport
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DNA-Binding Proteins
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Enzyme Inhibitors
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HIF1A protein, human
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Hypoxia-Inducible Factor 1
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Hypoxia-Inducible Factor 1, alpha Subunit
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Nuclear Proteins
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Proteins
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Pyrazoles
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Pyrimidines
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SHC1 protein, human
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Shc Signaling Adaptor Proteins
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Src Homology 2 Domain-Containing, Transforming Protein 1
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Transcription Factors
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Tyrphostins
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Ubiquitin
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6,7-dimethoxy-3-phenylquinoxaline
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Cobalt
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Cycloheximide
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src-Family Kinases
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Proto-Oncogene Proteins c-raf
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ras Proteins
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cobaltous chloride