Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.

Journal article

The (thio)carboxanilide derivatives are potent and selective inhibitors of HIV-1 reverse transcriptase (RT) and have a favourable antiviral activity spectrum. To understand better their mode of action, and to provide a structural basis for further improvement, models of RT complexed with four (thio)carboxanilide inhibitors (UC781, UC10, UC38 and UC84) have been constructed based on the X-ray structure of RT complexed with 9-chloro-TIBO. In the models, the protein conformation is similar to th...

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Authors: Esnouf, R; Stuart, D; De Clercq, E; Schwartz, E; Balzarini, J

• Publication status: Published
• Journal: Biochemical and biophysical research communications
• Volume: 234
• Issue: 2
• Pages: 458-464
• Publication date: 1997-05-01
• DOI: 10.1006/bbrc.1997.6552
• EISSN: 1090-2104
• ISSN: 0006-291X
• Language: English
• Keywords: Reverse Transcriptase Inhibitors; HIV-1; Drug Design; Carboxin; Imidazoles; Structure-Activity Relationship; Benzodiazepines; HIV Reverse Transcriptase; Models, Molecular; Anilides; Protein Conformation; Furans