| Literature DB >> 20438081 |
Eric B Lansdon1, Katherine M Brendza, Magdeleine Hung, Ruth Wang, Susmith Mukund, Debi Jin, Gabriel Birkus, Nilima Kutty, Xiaohong Liu.
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.Entities:
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Year: 2010 PMID： 20438081 DOI： 10.1021/jm1002233
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446