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. 2010 May 27;53(10):4295-9.
doi: 10.1021/jm1002233.

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

Eric B Lansdon  1 , Katherine M Brendza, Magdeleine Hung, Ruth Wang, Susmith Mukund, Debi Jin, Gabriel Birkus, Nilima Kutty, Xiaohong Liu
Affiliations

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

Eric B Lansdon et al. J Med Chem. .

Abstract

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 wild-type or K103N RT. Comparison to previously published structures reveals differences in binding modes for TMC125 and differences in protein conformation for TMC278.

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