Abstract
Tyrosylprotein sulfotransferases (TPSTs) catalyze the sulfation of tyrosine residues within secreted and membrane-bound proteins. The modification modulates protein-protein interactions in the extracellular environment. Here we use combinatorial target-guided ligand assembly to discover the first known inhibitors of human TPST-2.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Aldehydes / chemistry
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Combinatorial Chemistry Techniques
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Cytosol / drug effects
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Cytosol / enzymology
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Indicators and Reagents
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Ligands
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Sulfotransferases / antagonists & inhibitors*
Substances
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Aldehydes
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Enzyme Inhibitors
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Indicators and Reagents
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Ligands
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Sulfotransferases
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protein-tyrosine sulfotransferase
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estrone sulfotransferase