2a4r: Difference between revisions

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[[Image:2a4r.gif|left|200px]]
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{{STRUCTURE_2a4r|  PDB=2a4r  |  SCENE=  }}  
{{STRUCTURE_2a4r|  PDB=2a4r  |  SCENE=  }}  


'''HCV NS3 Protease Domain with a Ketoamide Inhibitor Covalently bound.'''
===HCV NS3 Protease Domain with a Ketoamide Inhibitor Covalently bound.===




==Overview==
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Modification of the P(2) and P(1) side chains of earlier P(3)-capped alpha-ketoamide inhibitor of HCV NS3 serine protease 1 resulted in the discovery of compound 24 with about 10-fold improvement in potency.
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{{ABSTRACT_PUBMED_16112862}}


==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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]
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]
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]
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency., Arasappan A, Njoroge FG, Chan TY, Bennett F, Bogen SL, Chen K, Gu H, Hong L, Jao E, Liu YT, Lovey RG, Parekh T, Pike RE, Pinto P, Santhanam B, Venkatraman S, Vaccaro H, Wang H, Yang X, Zhu Z, Mckittrick B, Saksena AK, Girijavallabhan V, Pichardo J, Butkiewicz N, Ingram R, Malcolm B, Prongay A, Yao N, Marten B, Madison V, Kemp S, Levy O, Lim-Wilby M, Tamura S, Ganguly AK, Bioorg Med Chem Lett. 2005 Oct 1;15(19):4180-4. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16087332 16087332]
The crystal structure of hepatitis C virus NS3 proteinase reveals a trypsin-like fold and a structural zinc binding site., Love RA, Parge HE, Wickersham JA, Hostomsky Z, Habuka N, Moomaw EW, Adachi T, Hostomska Z, Cell. 1996 Oct 18;87(2):331-42. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/8861916 8861916]
Complex of NS3 protease and NS4A peptide of BK strain hepatitis C virus: a 2.2 A resolution structure in a hexagonal crystal form., Yan Y, Li Y, Munshi S, Sardana V, Cole JL, Sardana M, Steinkuehler C, Tomei L, De Francesco R, Kuo LC, Chen Z, Protein Sci. 1998 Apr;7(4):837-47. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/9568891 9568891]
Inhibition of the hepatitis C virus NS3/4A protease. The crystal structures of two protease-inhibitor complexes., Di Marco S, Rizzi M, Volpari C, Walsh MA, Narjes F, Colarusso S, De Francesco R, Matassa VG, Sollazzo M, J Biol Chem. 2000 Mar 10;275(10):7152-7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/10702283 10702283]
[[Category: Hepatitis c virus]]
[[Category: Hepatitis c virus]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Saksena, A K.]]
[[Category: Saksena, A K.]]
[[Category: Virus/viral protein]]
[[Category: Virus/viral protein]]
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