1tkt
From Proteopedia
(New page: 200px<br /> <applet load="1tkt" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tkt, resolution 2.60Å" /> '''CRYSTAL STRUCTURE O...) |
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| - | [[Image:1tkt. | + | [[Image:1tkt.jpg|left|200px]]<br /><applet load="1tkt" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1tkt, resolution 2.60Å" /> | caption="1tkt, resolution 2.60Å" /> | ||
'''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318'''<br /> | '''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1TKT 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, MG and H12 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:// | + | 1TKT 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>, <scene name='pdbligand=MG:'>MG</scene> and <scene name='pdbligand=H12:'>H12</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=1TKT 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 16:57:27 2008'' |
Revision as of 14:57, 15 February 2008
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CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318
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
1TKT 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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