Abstract
Hydroxylation of hypoxia-inducible factor, a nuclear transcription factor, is catalysed by iron and 2-oxoglutarate dependent hydroxylases. Various analogues of the 2-oxoglutarate cosubstrate were synthesised and shown to inhibit the activity of human hypoxia-inducible factor-1alpha prolyl hydroxylases in cell-free extracts.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Catalysis
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Cell-Free System
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit
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Iron / chemistry
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Iron Chelating Agents / pharmacology
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Isoenzymes / antagonists & inhibitors
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Ketoglutaric Acids / chemical synthesis*
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Ketoglutaric Acids / pharmacology
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Molecular Structure
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Procollagen-Proline Dioxygenase / antagonists & inhibitors*
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Transcription Factors / metabolism*
Substances
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Enzyme Inhibitors
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HIF1A protein, human
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Hypoxia-Inducible Factor 1, alpha Subunit
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Iron Chelating Agents
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Isoenzymes
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Ketoglutaric Acids
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Transcription Factors
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Iron
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Procollagen-Proline Dioxygenase