2a4r
From Proteopedia
(New page: 200px<br /><applet load="2a4r" size="350" color="white" frame="true" align="right" spinBox="true" caption="2a4r, resolution 2.40Å" /> '''HCV NS3 Protease Dom...) |
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==Overview== | ==Overview== | ||
| - | Modification of the P(2) and P(1) side chains of earlier P(3)-capped | + | 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. |
==About this Structure== | ==About this Structure== | ||
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[[Category: Gu, H.]] | [[Category: Gu, H.]] | ||
[[Category: Madison, V.]] | [[Category: Madison, V.]] | ||
| - | [[Category: Njoroge, F | + | [[Category: Njoroge, F G.]] |
[[Category: Pichardo, J.]] | [[Category: Pichardo, J.]] | ||
[[Category: Prongay, A.]] | [[Category: Prongay, A.]] | ||
| - | [[Category: Saksena, A | + | [[Category: Saksena, A K.]] |
[[Category: BNH]] | [[Category: BNH]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
[[Category: virus/viral protein]] | [[Category: virus/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 16:23:35 2008'' |
Revision as of 14:23, 21 February 2008
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HCV NS3 Protease Domain with a Ketoamide Inhibitor Covalently bound.
Overview
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.
About this Structure
2A4R is a Protein complex structure of sequences from Hepatitis c virus with and as ligands. Full crystallographic information is available from OCA.
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:16112862
Page seeded by OCA on Thu Feb 21 16:23:35 2008
