Abstract
The structure-based design and synthesis of lactam-constrained azapeptide inhibitors of human cathepsin K are described. Enhanced stability to proteolytic cleavage over acyclic analogues is discussed.
MeSH terms
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Amines / chemistry
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Cathepsin K
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Cathepsins / antagonists & inhibitors*
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Cathepsins / metabolism
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Crystallography, X-Ray
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Cysteine Proteinase Inhibitors / chemical synthesis*
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Cysteine Proteinase Inhibitors / metabolism
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Cysteine Proteinase Inhibitors / pharmacology*
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Drug Design
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Humans
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Models, Molecular
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Osteoclasts / enzymology*
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Peptides / chemistry
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Pyrrolidinones / chemical synthesis*
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Pyrrolidinones / metabolism
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Pyrrolidinones / pharmacology
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Structure-Activity Relationship
Substances
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Amines
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Cysteine Proteinase Inhibitors
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Peptides
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Pyrrolidinones
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diaminopyrrolidinone
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Cathepsins
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CTSK protein, human
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Cathepsin K