1tkt
From Proteopedia
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[[Image:1tkt.jpg|left|200px]] | [[Image:1tkt.jpg|left|200px]] | ||
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'''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318''' | '''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318''' | ||
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[[Category: Stammers, D K.]] | [[Category: Stammers, D K.]] | ||
[[Category: Stuart, D I.]] | [[Category: Stuart, D I.]] | ||
- | [[Category: | + | [[Category: Aid]] |
- | [[Category: | + | [[Category: Drug design]] |
- | [[Category: | + | [[Category: Gw426318]] |
- | [[Category: | + | [[Category: Hiv-1 reverse transcriptase]] |
- | [[Category: | + | [[Category: Nnrti]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:04:24 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 07:04, 3 May 2008
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. 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 Page seeded by OCA on Sat May 3 10:04:24 2008