Abstract
An approach for the synthesis of carbonic anhydrase (CA, EC 4.2.1.1) inhibitor coated gold nanoparticles is reported. This nanomaterial selectively inhibited the tumor-associated isoform CA IX overexpressed in hypoxic cancers over the ubiquitous, cytosolic housekeeping isozymes CA I and II and was membrane impermeant. As CA IX has an extracellular active site, the new nanomaterial which is confined to the extracellular space may be useful for imaging and treatment of hypoxic tumors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / chemistry*
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Carbonic Anhydrase Inhibitors / pharmacology*
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Carbonic Anhydrases / metabolism*
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Cytosol / drug effects
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Cytosol / enzymology*
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Gold / chemistry*
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Humans
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / metabolism
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Metal Nanoparticles / chemistry*
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Molecular Structure
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Neoplasms / enzymology*
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Substrate Specificity
Substances
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Carbonic Anhydrase Inhibitors
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Isoenzymes
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Gold
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Carbonic Anhydrases