2qiq
From Proteopedia
(New page: 200px<br /><applet load="2qiq" size="350" color="white" frame="true" align="right" spinBox="true" caption="2qiq, resolution 1.900Å" /> '''Structure-based Des...) |
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==Overview== | ==Overview== | ||
| - | Structure-based design, synthesis, and biological evaluation of a series | + | Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors are 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 P(4)-ligand resulted in enhanced SARS-CoV 3CLpro inhibitory activity. Structural analysis of the inhibitor-bound X-ray structure revealed high binding affinity toward the enzyme. |
==About this Structure== | ==About this Structure== | ||
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[[Category: viral protein]] | [[Category: viral protein]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:39:43 2008'' |
Revision as of 16:39, 21 February 2008
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Structure-based Design and Synthesis and Biological Evaluation of Peptidomimetic SARS-3CLpro Inhibitors
Overview
Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors are 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 P(4)-ligand resulted in enhanced SARS-CoV 3CLpro inhibitory activity. Structural analysis of the inhibitor-bound X-ray structure revealed high binding affinity toward the enzyme.
About this Structure
2QIQ is a Single protein structure of sequence from Sars coronavirus with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors., Ghosh AK, Xi K, Grum-Tokars V, Xu X, Ratia K, Fu W, Houser KV, Baker SC, Johnson ME, Mesecar AD, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5876-80. Epub 2007 Aug 19. PMID:17855091
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