1rgq: Difference between revisions

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[[Image:1rgq.gif|left|200px]]
{{Seed}}
[[Image:1rgq.png|left|200px]]


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{{STRUCTURE_1rgq|  PDB=1rgq  |  SCENE=  }}  
{{STRUCTURE_1rgq|  PDB=1rgq  |  SCENE=  }}  


'''M9A HCV Protease complex with pentapeptide keto-amide inhibitor'''
===M9A HCV Protease complex with pentapeptide keto-amide inhibitor===




==Overview==
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A series of novel peptidyl-alpha-ketoamide compounds were evaluated as inhibitors of the deltaNS3-NS4A serine protease from the hepatitis C virus. These peptidyl-alpha-ketoamide inhibitors with Ki values ranging from 0.17 nM to 5.6 microM exhibited slow-binding inhibition. Kinetic studies established one-step kinetic mechanisms and dissociation rate constants in the 3-7 x 10(-5) s(-1) range for these compounds. The association rate constants, which ranged from 10 to 263,000 M(-1) s(-1), were responsible for the greater than four order of magnitude overall binding affinity range exhibited by this series. An X-ray crystal structure of a protease-inhibitor complex revealed an unusual interaction between the oxyanion of the adduct and the protein as well as a significant movement in the S1' region of the protein loop comprising residues 35-42. These results are quite different from peptidyl-alpha-ketoacid inhibition of HCV protease, which reportedly undergoes no notable conformational changes and proceeds with a two-step slow-binding kinetic mechanism.
The line below this paragraph, {{ABSTRACT_PUBMED_14984200}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_14984200}}


==About this Structure==
==About this Structure==
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[[Category: Stoll, V S.]]
[[Category: Stoll, V S.]]
[[Category: Hepatitis c virus protease keto amide peptide inhibitor]]
[[Category: Hepatitis c virus protease keto amide peptide inhibitor]]
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