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.

G., M., Radi, M., M., G., Botta, M., E., E. (2010). HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate. VIRUSES, 2, 880-899 [10.3390/v2040880].

HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate

RADI, MARCO;BOTTA, MAURIZIO;
2010-01-01

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.
G., M., Radi, M., M., G., Botta, M., E., E. (2010). HIV-1 RT inhibitors with a novel mechanism of action: NNRTIs that compete with the nucleotide substrate. VIRUSES, 2, 880-899 [10.3390/v2040880].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/20924
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