2f9u

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[[Image:2f9u.gif|left|200px]]
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{{Seed}}
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[[Image:2f9u.png|left|200px]]
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{{STRUCTURE_2f9u| PDB=2f9u | SCENE= }}
{{STRUCTURE_2f9u| PDB=2f9u | SCENE= }}
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'''HCV NS3 protease domain with NS4a peptide and a ketoamide inhibitor with a P2 norborane'''
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===HCV NS3 protease domain with NS4a peptide and a ketoamide inhibitor with a P2 norborane===
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==Overview==
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Prolonged hepatitis C infection is the leading cause for cirrhosis of the liver and hepatocellular carcinoma. The etiological agent HCV virus codes a single polyprotein of approximately 3000 amino acids that is processed with the help of a serine protease NS3A to produce structural and non-structural proteins required for viral replication. Inhibition of NS3 protease can potentially be used to develop drugs for treatment of HCV infections. Herein, we report the development of a series of novel NS3 serine protease inhibitors derived from 2-aza-bicyclo[2.2.1]-heptane carboxylic acid with potential therapeutic use for treatment of HCV infections.
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The line below this paragraph, {{ABSTRACT_PUBMED_16413182}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16413182 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16413182}}
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid., Venkatraman S, Njoroge FG, Wu W, Girijavallabhan V, Prongay AJ, Butkiewicz N, Pichardo J, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1628-32. Epub 2006 Jan 18. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16413182 16413182]
Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid., Venkatraman S, Njoroge FG, Wu W, Girijavallabhan V, Prongay AJ, Butkiewicz N, Pichardo J, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1628-32. Epub 2006 Jan 18. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16413182 16413182]
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Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide., Kim JL, Morgenstern KA, Lin C, Fox T, Dwyer MD, Landro JA, Chambers SP, Markland W, Lepre CA, O'Malley ET, Harbeson SL, Rice CM, Murcko MA, Caron PR, Thomson JA, Cell. 1996 Oct 18;87(2):343-55. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/8861917 8861917]
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Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency., Bogen S, Saksena AK, Arasappan A, Gu H, Njoroge FG, Girijavallabhan V, Pichardo J, Butkiewicz N, Prongay A, Madison V, Bioorg Med Chem Lett. 2005 Oct 15;15(20):4515-9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16112862 16112862]
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Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design., Venkatraman S, Njoroge FG, Girijavallabhan VM, Madison VS, Yao NH, Prongay AJ, Butkiewicz N, Pichardo J, J Med Chem. 2005 Aug 11;48(16):5088-91. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16078825 16078825]
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Proline-based macrocyclic inhibitors of the hepatitis C virus: stereoselective synthesis and biological activity., Chen KX, Njoroge FG, Vibulbhan B, Prongay A, Pichardo J, Madison V, Buevich A, Chan TM, Angew Chem Int Ed Engl. 2005 Nov 4;44(43):7024-8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16211639 16211639]
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Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex., Arasappan A, Njoroge FG, Parekh TN, Yang X, Pichardo J, Butkiewicz N, Prongay A, Yao N, Girijavallabhan V, Bioorg Med Chem Lett. 2004 Dec 6;14(23):5751-5. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15501035 15501035]
[[Category: Hepatitis c virus]]
[[Category: Hepatitis c virus]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Ketoamide inhibitor]]
[[Category: Ketoamide inhibitor]]
[[Category: Ns3 protease]]
[[Category: Ns3 protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:38:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 13:58:54 2008''

Revision as of 10:58, 27 July 2008

Image:2f9u.png

Template:STRUCTURE 2f9u

HCV NS3 protease domain with NS4a peptide and a ketoamide inhibitor with a P2 norborane

Template:ABSTRACT PUBMED 16413182

About this Structure

2F9U is a Protein complex structure of sequences from Hepatitis c virus. Full crystallographic information is available from OCA.

Reference

Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid., Venkatraman S, Njoroge FG, Wu W, Girijavallabhan V, Prongay AJ, Butkiewicz N, Pichardo J, Bioorg Med Chem Lett. 2006 Mar 15;16(6):1628-32. Epub 2006 Jan 18. PMID:16413182

Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide., Kim JL, Morgenstern KA, Lin C, Fox T, Dwyer MD, Landro JA, Chambers SP, Markland W, Lepre CA, O'Malley ET, Harbeson SL, Rice CM, Murcko MA, Caron PR, Thomson JA, Cell. 1996 Oct 18;87(2):343-55. PMID:8861917

Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency., Bogen S, Saksena AK, Arasappan A, Gu H, Njoroge FG, Girijavallabhan V, Pichardo J, Butkiewicz N, Prongay A, Madison V, Bioorg Med Chem Lett. 2005 Oct 15;15(20):4515-9. PMID:16112862

Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design., Venkatraman S, Njoroge FG, Girijavallabhan VM, Madison VS, Yao NH, Prongay AJ, Butkiewicz N, Pichardo J, J Med Chem. 2005 Aug 11;48(16):5088-91. PMID:16078825

Proline-based macrocyclic inhibitors of the hepatitis C virus: stereoselective synthesis and biological activity., Chen KX, Njoroge FG, Vibulbhan B, Prongay A, Pichardo J, Madison V, Buevich A, Chan TM, Angew Chem Int Ed Engl. 2005 Nov 4;44(43):7024-8. PMID:16211639

Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex., Arasappan A, Njoroge FG, Parekh TN, Yang X, Pichardo J, Butkiewicz N, Prongay A, Yao N, Girijavallabhan V, Bioorg Med Chem Lett. 2004 Dec 6;14(23):5751-5. PMID:15501035

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