Abstract
Aryl hydroxylamine derivatives have been synthesised that are some of the most potent inhibitors of hCMV protease prepared to date (IC50 14-60 nM). Mass spectrometry studies indicate that oxazinone derived hydroxylamines inhibit the enzyme by acylation of Ser132 whereas non-oxazinone derived hydroxylamines appear to inhibit via formation of a sulfinanilide at Cys138.
MeSH terms
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Amino Acid Sequence
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Anti-Infective Agents / chemical synthesis*
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Anti-Infective Agents / pharmacology
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Binding Sites
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Cytomegalovirus / enzymology*
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Cytomegalovirus Infections
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Humans
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Hydroxylamines / chemical synthesis*
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Hydroxylamines / pharmacology
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Mass Spectrometry
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Molecular Sequence Data
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Molecular Structure
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Peptide Fragments / chemistry
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Serine Endopeptidases / metabolism*
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / pharmacology
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Trypsin
Substances
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Anti-Infective Agents
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Hydroxylamines
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Peptide Fragments
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Serine Proteinase Inhibitors
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Serine Endopeptidases
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assemblin
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Trypsin