Next Article in Journal
HIV-1 Ribonuclease H: Structure, Catalytic Mechanism and Inhibitors
Next Article in Special Issue
HIV-1 Entry, Inhibitors, and Resistance
Previous Article in Journal
The Effect of Antiretroviral Combination Treatment on Epstein-Barr Virus (EBV) Genome Load in HIV-Infected Patients
Previous Article in Special Issue
HIV Genetic Diversity and Drug Resistance
Viruses 2010, 2(4), 880-899; doi:10.3390/v2040880

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 / Revised: 20 February 2010 / Accepted: 5 March 2010 / Published: 30 March 2010
(This article belongs to the Special Issue HIV Drug Resistance 2010)
View Full-Text   |   Download PDF [888 KB, uploaded 12 May 2015]   |   Browse Figures


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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here


[Return to top]
Viruses EISSN 1999-4915 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert