Author: Ghosh, Arun K.; Xi, Kai; Grum-Tokars, Valerie; Xu, Xiaoming; Ratia, Kiira; Fu, Wentao; Houser, Katherine V.; Baker, Susan C.; Johnson, Michael E.; Mesecar, Andrew D.
Title: Structure-based Design, Synthesis and Biological Evaluation of Peptidomimetic SARS-CoV 3CLpro Inhibitors Cord-id: lfhy70b5 Document date: 2007_11_1
ID: lfhy70b5
Snippet: Structure-based design, synthesis and biological evaluation of a series of peptidomimetic severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors is described. These inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 1 bound to SARS-CoV 3CLpro. Incorporation of Boc-Ser as the P4-ligand resulted in enhanced SARS-CoV 3CLpro inhibitory activity. Structural analysis of inhibitor-bound X-ray structure revealed high binding affinity
Document: Structure-based design, synthesis and biological evaluation of a series of peptidomimetic severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors is described. These inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 1 bound to SARS-CoV 3CLpro. Incorporation of Boc-Ser as the P4-ligand resulted in enhanced SARS-CoV 3CLpro inhibitory activity. Structural analysis of inhibitor-bound X-ray structure revealed high binding affinity towards the enzyme.
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