Crystal structures of HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278): implications for drug design.
J Med Chem
; 53(10): 4295-9, 2010 May 27.
Article
em En
| MEDLINE
| ID: mdl-20438081
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridazinas
/
Pirimidinas
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Desenho de Fármacos
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HIV-1
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Transcriptase Reversa do HIV
/
Nitrilas
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article