Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.

Abstract:

We have used a structure-based approach to design a novel series of ...
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.

Polymerases:

Topics:

Health/Disease, Structure and Structure/Function, Reverse Transcriptase

Status:

new topics/pols set partial results complete validated

Results:

Polymerase Reference Property Result Context
HIV RT Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1. Reverse Transcriptase Activity Yes
HIV RT Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1. Associated condition HIV

Structures:

1TL3 1TL1 1TKZ 1TKT

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