Abstract
Polyoxotungstates were identified as potent inhibitors of NTPDases1, 2, and 3. The most potent compound was K(6)H(2)[TiW(11)CoO(40)], exhibiting K(i) values of 0.140 microM (NTPDase1), 0.910 microM (NTPDase2), and 0.563 microM (NTPDase3). One of the compounds, (NH(4))(18)[NaSb(9)W(21)O(86)], was selective for NTPDases2 and 3 versus NTPDase1. NTPDase inhibition might contribute to the described biological effects of polyoxometalates, including their anti-cancer activity.
MeSH terms
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Adenosine Triphosphatases / antagonists & inhibitors*
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Adenosine Triphosphatases / metabolism
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Animals
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Antigens, CD / metabolism
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Apyrase / antagonists & inhibitors*
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Apyrase / metabolism
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / classification*
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Enzyme Inhibitors / pharmacology*
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Models, Molecular
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Molecular Structure
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Pyrophosphatases / antagonists & inhibitors*
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Pyrophosphatases / metabolism
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Rats
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Structure-Activity Relationship
Substances
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Antigens, CD
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Enzyme Inhibitors
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Adenosine Triphosphatases
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Pyrophosphatases
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ectoATPase
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nucleoside-triphosphate diphosphohydrolase 3
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Apyrase
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CD39 antigen