1tkt

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{{STRUCTURE_1tkt| PDB=1tkt | SCENE= }}
{{STRUCTURE_1tkt| PDB=1tkt | SCENE= }}
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'''CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318'''
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===CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 15537346 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15537346}}
==About this Structure==
==About this Structure==
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[[Category: Hiv-1 reverse transcriptase]]
[[Category: Hiv-1 reverse transcriptase]]
[[Category: Nnrti]]
[[Category: Nnrti]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:30:33 2008''

Revision as of 16:30, 28 July 2008

Image:1tkt.png

Template:STRUCTURE 1tkt

CRYSTAL STRUCTURE OF HIV-1 REVERSE TRANSCRIPTASE IN COMPLEX WITH GW426318

Template:ABSTRACT PUBMED 15537346

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

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