Abstract
Using our recently disclosed fluorescence-based assay to monitor acyltransferase activity, the first non-peptidic, small molecule antagonists of ghrelin O-acyltransferase (GOAT), a potential anti-obesity and anti-diabetes target, have been discovered. Each exhibits micromolar inhibition of the enzyme, and may be useful probes for future study of the ghrelin-GOAT system.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Acyltransferases / antagonists & inhibitors*
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Acyltransferases / chemistry
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Acyltransferases / metabolism*
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Amino Acid Sequence
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / pharmacology*
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Ghrelin / metabolism*
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Molecular Sequence Data
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Small Molecule Libraries / pharmacology*
Substances
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Enzyme Inhibitors
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Ghrelin
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Small Molecule Libraries
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Acyltransferases