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Article

High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.

Proceedings of the National Academy of Sciences of the United States of America - 5 Feb 2008

Das Kalyan, Bauman Joseph D, Clark Arthur D, Frenkel Yulia V, Lewi Paul J, Shatkin Aaron J, Hughes Stephen H, Arnold Eddy

Abstract excerpt

TMC278 is a diarylpyrimidine (DAPY) nonnucleoside reverse transcriptase inhibitor (NNRTI) that is highly effective in treating wild-type and drug-resistant HIV-1 infections in clinical trials at relatively low doses ( approximately 25-75 mg/day). We have determined the structure of wild-type HIV-1 RT complexed with TMC278 at 1.8 A resolution, using an RT crystal form engineered by systematic RT mutagenesis. This...

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Identifiers

PMID: 18230722
DOI: 10.1073/pnas.0711209105
PMCID: PMC2234167

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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