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

Giovanni Maga, Marco Radi, M. Gerard, Maurizio Botta, Eric Ennifar
Published 2010 in Viruses

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… (More)

DOI: 10.3390/v2040880

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).

Paul A J Janssen, Paul J Lewi, +23 authors Paul Stoffels
Journal of medicinal chemistry
2005

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

Abstract

Topics

11 Figures and Tables

Cited By

Computational drug design strategies applied to the modelling of human immunodeficiency virus-1 reverse transcriptase inhibitors

How to win the HIV-1 drug resistance hurdle race: running faster or jumping higher?

Potential of small-molecule fungal metabolites in antiviral chemotherapy.

Drug design strategies using non nucleoside reverse transcriptase inhibitors (NNRTI): current challenges and future perspectives

Characterization of antiviral activity of benzamide derivative AH0109 against HIV-1 infection.

Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor series.

Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.

Synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents.

References

Mutations M184V and Y115F in HIV-1 reverse transcriptase discriminate against "nucleotide-competing reverse transcriptase inhibitors".

Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action.

Novel nonnucleoside inhibitors that select nucleoside inhibitor resistance mutations in human immunodeficiency virus type 1 reverse transcriptase.

High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.

Antagonism between the HIV-1 reverse-transcriptase mutation K65R and thymidine-analogue mutations at the genomic level.

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).

Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance.

3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.

Efficacy and safety of etravirine in treatment-experienced, HIV-1 patients: pooled 48 week analysis of two randomized, controlled trials.

Mutation Rates and Intrinsic Fidelity of Retroviral Reverse Transcriptases

Slides referencing similar topics

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

Abstract

Topics

11 Figures and Tables

Cited By

Computational drug design strategies applied to the modelling of human immunodeficiency virus-1 reverse transcriptase inhibitors

How to win the HIV-1 drug resistance hurdle race: running faster or jumping higher?

Potential of small-molecule fungal metabolites in antiviral chemotherapy.

Drug design strategies using non nucleoside reverse transcriptase inhibitors (NNRTI): current challenges and future perspectives

Characterization of antiviral activity of benzamide derivative AH0109 against HIV-1 infection.

Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor series.

Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.

Synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents.

References

Mutations M184V and Y115F in HIV-1 reverse transcriptase discriminate against "nucleotide-competing reverse transcriptase inhibitors".

Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action.

Novel nonnucleoside inhibitors that select nucleoside inhibitor resistance mutations in human immunodeficiency virus type 1 reverse transcriptase.

High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations.

Antagonism between the HIV-1 reverse-transcriptase mutation K65R and thymidine-analogue mutations at the genomic level.

In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).

Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: implications for drug resistance.

3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.

Efficacy and safety of etravirine in treatment-experienced, HIV-1 patients: pooled 48 week analysis of two randomized, controlled trials.

Mutation Rates and Intrinsic Fidelity of Retroviral Reverse Transcriptases

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