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Viruses 2010, 2(4), 880-899; doi:10.3390/v2040880
Review

HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate

1
,
2
,
3
,
2
 and
3,*
1 Istituto di Genetica Molecolare, IGM-CNR, Via Abiategrasso 207, 27100 Pavia, Italy 2 Dipartimento Farmaco Chimico Tecnologico, University of Siena, Via Alcide de Gasperi 2, 53100 Siena, Italy 3 Architecture et Réactivité des ARN, Université de Strasbourg, CNRS, 15 rue René Descartes, F-67084 Strasbourg, France
* Author to whom correspondence should be addressed.
Received: 22 January 2010 / Revised: 20 February 2010 / Accepted: 5 March 2010 / Published: 30 March 2010
(This article belongs to the Special Issue HIV Drug Resistance 2010)
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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.
Keywords: HIV; reverse transcriptase; competitive inhibitors HIV; reverse transcriptase; competitive inhibitors
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Maga, G.; Radi, M.; Gerard, M.-A.; Botta, M.; Ennifar, E. HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate. Viruses 2010, 2, 880-899.

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