2hwi

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|PDB= 2hwi |SIZE=350|CAPTION= <scene name='initialview01'>2hwi</scene>, resolution 2.0&Aring;
|PDB= 2hwi |SIZE=350|CAPTION= <scene name='initialview01'>2hwi</scene>, resolution 2.0&Aring;
|SITE=
|SITE=
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|LIGAND= <scene name='pdbligand=VRX:(2S)-({(5Z)-5-[(5-ETHYL-2-FURYL)METHYLENE]-4-OXO-4,5-DIHYDRO-1,3-THIAZOL-2-YL}AMINO)(4-FLUOROPHENYL)ACETIC ACID'>VRX</scene>
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|LIGAND= <scene name='pdbligand=VRX:(2S)-({(5Z)-5-[(5-ETHYL-2-FURYL)METHYLENE]-4-OXO-4,5-DIHYDRO-1,3-THIAZOL-2-YL}AMINO)(4-FLUOROPHENYL)ACETIC+ACID'>VRX</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48]
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/RNA-directed_RNA_polymerase RNA-directed RNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.48 2.7.7.48] </span>
|GENE=
|GENE=
 +
|DOMAIN=
 +
|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hwi OCA], [http://www.ebi.ac.uk/pdbsum/2hwi PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hwi RCSB]</span>
}}
}}
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Yao, N.]]
[[Category: Yao, N.]]
-
[[Category: VRX]]
 
[[Category: allosteric inhibitor]]
[[Category: allosteric inhibitor]]
[[Category: hcv]]
[[Category: hcv]]
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[[Category: viral rna-directed rna polymerase]]
[[Category: viral rna-directed rna polymerase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:22:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:36:25 2008''

Revision as of 00:36, 31 March 2008


PDB ID 2hwi

Drag the structure with the mouse to rotate
, resolution 2.0Å
Ligands:
Activity: RNA-directed RNA polymerase, with EC number 2.7.7.48
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



HCV NS5B allosteric inhibitor complex


Overview

A structure-based approach was performed to design a novel thiazolone scaffold as HCV NS5B inhibitors. A focused library was designed and docked by GOLD. One of the top-scored molecules was synthesized and shown to have similar potency to the initial hit. The X-ray complex structure was determined and validated our design rationale.

About this Structure

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

Reference

Structure-based design of a novel thiazolone scaffold as HCV NS5B polymerase allosteric inhibitors., Yan S, Appleby T, Larson G, Wu JZ, Hamatake R, Hong Z, Yao N, Bioorg Med Chem Lett. 2006 Nov 15;16(22):5888-91. Epub 2006 Aug 24. PMID:16934455

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