Dipeptidyl nitrile inhibitors of Cathepsin L.

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

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.

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关键词

Cathepsin,Cathepsin B,Cathepsin K,Cathepsin L,Cathepsin L2,Cathepsin S,Cathepsin V,Cysteine protease,Nitrile,Covalent inhibitor,Selectivity,Protein structure,X-ray crystallography,Structure-based design,Molecular pincer,Conformational lock,Tautomeric lock,Osteoarthritis,Aggrecan,Collagen,Cartilage

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