A new class of non-nucleoside reverse transcriptase inhibitors with a 6-vinylpyrimidine scaffold (1) has been found to inhibit HIV-1 reverse transcriptase (RT) by competition with the nucleotide substrate after binding to the non-nucleoside inhibitor binding pocket of the enzyme. Molecular modeling studies have been performed to elucidate their peculiar behavior.
Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Competing with the Nucleotide Substrate / Giovanni, Maga; Radi, Marco; Samantha, Zanoli; Fabrizio, Manetti; Reynel, Cancio; Ulrich, Hübscher; Silvio, Spadari; Chiara, Falciani; Montserrat, Terrazas; Jaume, Vilarrasa; Maurizio, Botta. - In: ANGEWANDTE CHEMIE. INTERNATIONAL EDITION. - ISSN 1433-7851. - 46:(2007), pp. 1810-1813. [10.1002/anie.200604165]
Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Competing with the Nucleotide Substrate
RADI, Marco;
2007-01-01
Abstract
A new class of non-nucleoside reverse transcriptase inhibitors with a 6-vinylpyrimidine scaffold (1) has been found to inhibit HIV-1 reverse transcriptase (RT) by competition with the nucleotide substrate after binding to the non-nucleoside inhibitor binding pocket of the enzyme. Molecular modeling studies have been performed to elucidate their peculiar behavior.File | Dimensione | Formato | |
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