Abstract
We have determined a possible transition-state for the reaction catalysed by the enzyme Estrone Sulfatase (ES) - as a representation of the active site. Using the derived structure, we have superimposed several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors.
MeSH terms
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Binding Sites
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Catalysis
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology
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Models, Molecular
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Structure-Activity Relationship
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Substrate Specificity
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Sulfatases / antagonists & inhibitors
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Sulfatases / chemistry
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Sulfatases / metabolism*
Substances
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Enzyme Inhibitors
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Sulfatases
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estrone sulfatase