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Article

Crystal structures of HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278): implications for drug design.

Journal of medicinal chemistry - 27 May 2010

Lansdon Eric B, Brendza Katherine M, Hung Magdeleine, Wang Ruth, Mukund Susmith, Jin Debi, Birkus Gabriel, Kutty Nilima, Liu Xiaohong

Abstract excerpt

Diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitors (NNRTIs) have inherent flexibility, helping to maintain activity against a wide range of resistance mutations. Crystal structures were determined with wild-type and K103N HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278). These structures reveal a similar binding mode for TMC125 and TMC278, whether bound to...

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Identifiers

PMID: 20438081
DOI: 10.1021/jm1002233

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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