1rgq

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[[Image:1rgq.gif|left|200px]]
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{{Seed}}
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[[Image:1rgq.png|left|200px]]
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{{STRUCTURE_1rgq| PDB=1rgq | SCENE= }}
{{STRUCTURE_1rgq| PDB=1rgq | SCENE= }}
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'''M9A HCV Protease complex with pentapeptide keto-amide inhibitor'''
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===M9A HCV Protease complex with pentapeptide keto-amide inhibitor===
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==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.
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(as it appears on PubMed at http://www.pubmed.gov), where 14984200 is the PubMed ID number.
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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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:28:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:32:00 2008''

Revision as of 23:32, 27 July 2008

Image:1rgq.png

Template:STRUCTURE 1rgq

M9A HCV Protease complex with pentapeptide keto-amide inhibitor

Template:ABSTRACT PUBMED 14984200

About this Structure

1RGQ is a Protein complex structure of sequences from Hepatitis c virus. Full crystallographic information is available from OCA.

Reference

Hepatitis C NS3 protease inhibition by peptidyl-alpha-ketoamide inhibitors: kinetic mechanism and structure., Liu Y, Stoll VS, Richardson PL, Saldivar A, Klaus JL, Molla A, Kohlbrenner W, Kati WM, Arch Biochem Biophys. 2004 Jan 15;421(2):207-16. PMID:14984200

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