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HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate
Istituto di Genetica Molecolare, IGM-CNR, Via Abiategrasso 207, 27100 Pavia, Italy
Dipartimento Farmaco Chimico Tecnologico, University of Siena, Via Alcide de Gasperi 2, 53100 Siena, Italy
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; in revised form: 20 February 2010 / Accepted: 5 March 2010 / Published: 30 March 2010
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
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MDPI and ACS Style
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.
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(4):880-899.
Maga, Giovanni; Radi, Marco; Gerard, Marie-Aline; Botta, Maurizio; Ennifar, Eric. 2010. "HIV-1 RT Inhibitors with a Novel Mechanism of Action: NNRTIs that Compete with the Nucleotide Substrate." Viruses 2, no. 4: 880-899.