2gc8

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[[Image:2gc8.gif|left|200px]]
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{{STRUCTURE_2gc8| PDB=2gc8 | SCENE= }}
{{STRUCTURE_2gc8| PDB=2gc8 | SCENE= }}
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'''Structure of a Proline Sulfonamide Inhibitor Bound to HCV NS5b Polymerase'''
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===Structure of a Proline Sulfonamide Inhibitor Bound to HCV NS5b Polymerase===
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==Overview==
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Through high throughput screening, substituted proline sulfonamide 6 was identified as HCV NS5b RNA-dependent RNA polymerase inhibitor. Optimization of various regions of the lead molecule resulted in compounds that displayed good potency and selectivity. The crystal structure of 6 and NS5b polymerase complex confirmed the binding near the active site region. The optimization approach and SAR are discussed in detail.
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(as it appears on PubMed at http://www.pubmed.gov), where 16722622 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16722622}}
==About this Structure==
==About this Structure==
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[[Category: Connell, J O.]]
[[Category: Connell, J O.]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:56:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 02:06:41 2008''

Revision as of 23:07, 28 July 2008

Image:2gc8.png

Template:STRUCTURE 2gc8

Structure of a Proline Sulfonamide Inhibitor Bound to HCV NS5b Polymerase

Template:ABSTRACT PUBMED 16722622

About this Structure

2GC8 is a Single protein structure of sequence from Hepatitis c virus. Full crystallographic information is available from OCA.

Reference

Discovery of proline sulfonamides as potent and selective hepatitis C virus NS5b polymerase inhibitors. Evidence for a new NS5b polymerase binding site., Gopalsamy A, Chopra R, Lim K, Ciszewski G, Shi M, Curran KJ, Sukits SF, Svenson K, Bard J, Ellingboe JW, Agarwal A, Krishnamurthy G, Howe AY, Orlowski M, Feld B, O'Connell J, Mansour TS, J Med Chem. 2006 Jun 1;49(11):3052-5. PMID:16722622

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