1z4u
From Proteopedia
(New page: 200px<br /><applet load="1z4u" size="450" color="white" frame="true" align="right" spinBox="true" caption="1z4u, resolution 2.80Å" /> '''hepatitis C virus NS...) |
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- | [[Image:1z4u.gif|left|200px]]<br /><applet load="1z4u" size=" | + | [[Image:1z4u.gif|left|200px]]<br /><applet load="1z4u" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1z4u, resolution 2.80Å" /> | caption="1z4u, resolution 2.80Å" /> | ||
'''hepatitis C virus NS5B RNA-dependent RNA polymerase complex with inhibitor PHA-00799585'''<br /> | '''hepatitis C virus NS5B RNA-dependent RNA polymerase complex with inhibitor PHA-00799585'''<br /> | ||
==Overview== | ==Overview== | ||
- | A novel series of non-nucleoside HCV NS5B polymerase inhibitors was | + | A novel series of non-nucleoside HCV NS5B polymerase inhibitors was prepared from a (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid template. Solution and solid phase analog synthesis focused on the northern region of the template combined with structure based design led to the discovery of several potent and orally bioavailable lead compounds. |
==About this Structure== | ==About this Structure== | ||
- | 1Z4U is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with CL, PO4, PH9 and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | + | 1Z4U is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Hepatitis_c_virus Hepatitis c virus] with <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=PO4:'>PO4</scene>, <scene name='pdbligand=PH9:'>PH9</scene> and <scene name='pdbligand=GOL:'>GOL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Z4U OCA]. |
==Reference== | ==Reference== | ||
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[[Category: RNA-directed RNA polymerase]] | [[Category: RNA-directed RNA polymerase]] | ||
[[Category: Anstadt, R.]] | [[Category: Anstadt, R.]] | ||
- | [[Category: Finzel, B | + | [[Category: Finzel, B C.]] |
[[Category: Greene, M.]] | [[Category: Greene, M.]] | ||
- | [[Category: Gross, R | + | [[Category: Gross, R J.]] |
- | [[Category: Harris, M | + | [[Category: Harris, M S.]] |
- | [[Category: Mitchell, M | + | [[Category: Mitchell, M A.]] |
[[Category: Nugent, R.]] | [[Category: Nugent, R.]] | ||
- | [[Category: Pfefferkorn, J | + | [[Category: Pfefferkorn, J A.]] |
- | [[Category: Shelly, J | + | [[Category: Shelly, J A.]] |
- | [[Category: Wells, P | + | [[Category: Wells, P A.]] |
[[Category: CL]] | [[Category: CL]] | ||
[[Category: GOL]] | [[Category: GOL]] | ||
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[[Category: thumb]] | [[Category: thumb]] | ||
- | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:12:05 2008'' |
Revision as of 14:12, 21 February 2008
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hepatitis C virus NS5B RNA-dependent RNA polymerase complex with inhibitor PHA-00799585
Overview
A novel series of non-nucleoside HCV NS5B polymerase inhibitors was prepared from a (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid template. Solution and solid phase analog synthesis focused on the northern region of the template combined with structure based design led to the discovery of several potent and orally bioavailable lead compounds.
About this Structure
1Z4U is a Protein complex structure of sequences from Hepatitis c virus with , , and as ligands. Active as RNA-directed RNA polymerase, with EC number 2.7.7.48 Full crystallographic information is available from OCA.
Reference
Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid., Pfefferkorn JA, Nugent R, Gross RJ, Greene M, Mitchell MA, Reding MT, Funk LA, Anderson R, Wells PA, Shelly JA, Anstadt R, Finzel BC, Harris MS, Kilkuskie RE, Kopta LA, Schwende FJ, Bioorg Med Chem Lett. 2005 Jun 2;15(11):2812-8. PMID:15911260
Page seeded by OCA on Thu Feb 21 16:12:05 2008
Categories: Hepatitis c virus | Protein complex | RNA-directed RNA polymerase | Anstadt, R. | Finzel, B C. | Greene, M. | Gross, R J. | Harris, M S. | Mitchell, M A. | Nugent, R. | Pfefferkorn, J A. | Shelly, J A. | Wells, P A. | CL | GOL | PH9 | PO4 | Fingers | Hcv | Ns5b | Palm | Polymerase | Thumb