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Discovery of Non‐Nucleoside Inhibitors of HIV‐1 Reverse Transcriptase Competing with the Nucleotide Substrate
Author(s) -
Maga Giovanni,
Radi Marco,
Zanoli Samantha,
Manetti Fabrizio,
Cancio Reynel,
Hübscher Ulrich,
Spadari Silvio,
Falciani Chiara,
Terrazas Montserrat,
Vilarrasa Jaume,
Botta Maurizio
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200604165
Subject(s) - reverse transcriptase , nucleotide , nucleoside , substrate (aquarium) , nucleoside reverse transcriptase inhibitor , human immunodeficiency virus (hiv) , enzyme , chemistry , binding site , reverse transcriptase inhibitor , stereochemistry , biochemistry , biology , virology , rna , gene , ecology
How odd! 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.