Abstract
Structure-based design was utilized to guide the early stage optimization of a substrate-like inhibitor to afford potent peptidomimetic inhibitors of the channel-activating protease prostasin. The first X-ray crystal structures of prostasin with small molecule inhibitors bound to the active site are also reported.
MeSH terms
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Combinatorial Chemistry Techniques
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Crystallography, X-Ray
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Molecular Mimicry
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Molecular Structure
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Protein Conformation
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Serine Endopeptidases / drug effects*
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / chemistry
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Serine Proteinase Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Serine Proteinase Inhibitors
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Serine Endopeptidases
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prostasin