1tl3
From Proteopedia
(New page: 200px<br /> <applet load="1tl3" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tl3, resolution 2.80Å" /> '''Crystal structure o...) |
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| - | [[Image:1tl3.gif|left|200px]]<br /> | + | [[Image:1tl3.gif|left|200px]]<br /><applet load="1tl3" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1tl3, resolution 2.80Å" /> | caption="1tl3, resolution 2.80Å" /> | ||
'''Crystal structure of hiv-1 reverse transcriptase in complex with gw450557'''<br /> | '''Crystal structure of hiv-1 reverse transcriptase in complex with gw450557'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1TL3 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with PO4 and H20 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/RNA-directed_DNA_polymerase RNA-directed DNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.49 2.7.7.49] Full crystallographic information is available from [http:// | + | 1TL3 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Human_immunodeficiency_virus_1 Human immunodeficiency virus 1] with <scene name='pdbligand=PO4:'>PO4</scene> and <scene name='pdbligand=H20:'>H20</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/RNA-directed_DNA_polymerase RNA-directed DNA polymerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.7.49 2.7.7.49] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TL3 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: nnrti]] | [[Category: nnrti]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:57:33 2008'' |
Revision as of 14:57, 15 February 2008
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Crystal structure of hiv-1 reverse transcriptase in complex with gw450557
Overview
We have used a structure-based approach to design a novel series of, non-nucleoside inhibitors of HIV-1 RT (NNRTIs). Detailed analysis of a, wide range of crystal structures of HIV-1 RT-NNRTI complexes together with, data on drug resistance mutations has identified factors important for, tight binding of inhibitors and resilience to mutations. Using this, approach we have designed and synthesized a novel series of quinolone, NNRTIs. Crystal structure analysis of four of these compounds in complexes, with HIV-1 RT confirms the predicted binding modes. Members of this, quinolone series retain high activity against the important resistance, mutations in RT at Tyr181Cys and Leu100Ile.
About this Structure
1TL3 is a Protein complex structure of sequences from Human immunodeficiency virus 1 with and as ligands. Active as RNA-directed DNA polymerase, with EC number 2.7.7.49 Full crystallographic information is available from OCA.
Reference
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1., Hopkins AL, Ren J, Milton J, Hazen RJ, Chan JH, Stuart DI, Stammers DK, J Med Chem. 2004 Nov 18;47(24):5912-22. PMID:15537346
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