Abstract
A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.
MeSH terms
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Animals
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Cartilage, Articular / pathology
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Catalysis
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Cathepsin L / antagonists & inhibitors*
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Cathepsin L / chemistry*
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Chemistry, Pharmaceutical / methods
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Crystallography, X-Ray / methods
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Drug Design
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Humans
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Ligands
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Mice
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Mice, Transgenic
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Nitriles / chemical synthesis*
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Nitriles / chemistry
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Nitriles / pharmacology
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Peptides / chemical synthesis
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Peptides / pharmacology
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Proteins / chemistry
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Structure-Activity Relationship
Substances
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Ligands
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Nitriles
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Peptides
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Proteins
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Cathepsin L