Inhibition of Cathepsin L by Epoxysuccinyl Peptides Simultaneously Addressing Active-Site and Remote-Site Regions

The propeptide domain as structural guide: Based on information provided by the cathepsin L prodomain, a remote‐site region was identified and exploited to improve the affinity/selectivity profile of irreversible cathepsin L inhibitors.

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Bibliographische Detailangaben
Veröffentlicht in:	Chembiochem : a European journal of chemical biology 2008-07, Vol.9 (11), p.1721-1724
Hauptverfasser:	Schaschke, Norbert, Assfalg-Machleidt, Irmgard, Machleidt, Werner
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Binding Sites Cathepsin L Cathepsins - antagonists & inhibitors Cathepsins - chemistry Cathepsins - metabolism Crystallography, X-Ray Cysteine Endopeptidases - chemistry Cysteine Endopeptidases - metabolism cysteine protease E-64 Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans inhibitors Models, Molecular Molecular Sequence Data peptide-protein interactions Peptides - chemical synthesis Peptides - chemistry Peptides - pharmacology propeptides Protein Conformation Succinic Acid - chemistry
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Beschreibung
Zusammenfassung:	The propeptide domain as structural guide: Based on information provided by the cathepsin L prodomain, a remote‐site region was identified and exploited to improve the affinity/selectivity profile of irreversible cathepsin L inhibitors.
ISSN:	1439-4227 1439-7633
DOI:	10.1002/cbic.200800103