Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5794
Title: HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate
Authors: G., Maga
Radi, Marco
M., Gerard
Botta, Maurizio 
E., Ennifar
Keywords: HIV; reverse transcriptase; competitive inhibitors
Issue Date: 2010
Project: None 
Journal: VIRUSES
Abstract: 
HIV-1 reverse transcriptase (RT) inhibitors currently used in antiretroviral therapy can be divided into two classes: (i) nucleoside analog RT inhibitors (NRTIs), which compete with natural nucleoside substrates and act as terminators of proviral DNA synthesis, and (ii) non-nucleoside RT inhibitors (NNRTIs), which bind to a hydrophobic pocket close to the RT active site. In spite of the efficiency of NRTIs and NNRTIs, the rapid emergence of multidrug-resistant mutations requires the development of new RT inhibitors with an alternative mechanism of action. Recently, several studies reported the discovery of novel non-nucleoside inhibitors with a distinct mechanism of action. Unlike classical NNRTIs, they compete with the nucleotide substrate, thus forming a new class of RT inhibitors: nucleotide-competing RT inhibitors (NcRTIs). In this review, we discuss current progress in the understanding of the peculiar behavior of these compounds.
Description: 
22443
URI: http://hdl.handle.net/20.500.12779/5794
ISSN: 1999-4915
DOI: 10.3390/v2040880
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