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 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; in revised form: 20 February 2010 / Accepted: 5 March 2010 / Published: 30 March 2010
(This article belongs to the Special Issue HIV Drug Resistance)
PDF Full-text Download PDF Full-Text [888 KB, uploaded 30 March 2010 14:04 CEST]
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

Article Statistics

Load and display the download statistics.

Citations to this Article

Cite This Article

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.

AMA 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(4):880-899.

Chicago/Turabian Style

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.

Viruses EISSN 1999-4915 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert