Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor. (Q37467660)

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scientific article published on December 2009

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English	Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor.	scientific article published on December 2009

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10 February 2020

Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor (English)

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Stefan G. Sarafianos

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Eleftherios Michailidis

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Michael A Parniak

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Michael A Parniak

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Eva Nagy

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Emily M Ryan

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Hiroaki Mitsuya

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Hiroaki Mitsuya

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Noriyuki Ashida

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Noriyuki Ashida

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Bruno Marchand

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Kamlendra Singh

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Ali M Sawani

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1 December 2009

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Journal of Biological Chemistry

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35681-35691

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10 February 2020

Potent activity of a nucleoside reverse transcriptase inhibitor, 4'-ethynyl-2-fluoro-2'-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted NOD/SCID Janus kinase

1 reference

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Antimicrobial strategies: inhibition of viral polymerases by 3'-hydroxyl nucleosides

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23 August 2017

Structure and function of HIV-1 reverse transcriptase: molecular mechanisms of polymerization and inhibition

1 reference

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23 August 2017

2'-deoxy-4'-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants

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Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphate

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23 August 2017

Mechanisms of inhibition of HIV replication by non-nucleoside reverse transcriptase inhibitors

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23 August 2017

Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine

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23 August 2017

Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir

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23 August 2017

Comparison of the phosphorylation of 4'-ethynyl 2',3'-dihydro-3'-deoxythymidine with that of other anti-human immunodeficiency virus thymidine analogs.

1 reference

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Pharmacology of current and promising nucleosides for the treatment of human immunodeficiency viruses

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23 August 2017

Anti-human immunodeficiency virus type 1 activity and resistance profile of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine in vitro

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23 August 2017

Nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase

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23 August 2017

Relationship between antiviral activity and host toxicity: comparison of the incorporation efficiencies of 2',3'-dideoxy-5-fluoro-3'-thiacytidine-triphosphate analogs by human immunodeficiency virus type 1 reverse transcriptase and human mitochondri

1 reference

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23 August 2017

Structures of HIV-1 reverse transcriptase with pre- and post-translocation AZTMP-terminated DNA.

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23 August 2017

4'-C-substituted-2'-deoxynucleosides: a family of antiretroviral agents which are potent against drug-resistant HIV variants

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23 August 2017

Improving nucleoside diphosphate kinase for antiviral nucleotide analogs activation

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23 August 2017

4'-Ethynyl nucleoside analogs: potent inhibitors of multidrug-resistant human immunodeficiency virus variants in vitro

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23 August 2017

Molecular mechanisms of HIV-1 resistance to nucleoside reverse transcriptase inhibitors (NRTIs).

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23 August 2017

Inhibitors of HIV-1 reverse transcriptase

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23 August 2017

A mechanism of AZT resistance: an increase in nucleotide-dependent primer unblocking by mutant HIV-1 reverse transcriptase

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23 August 2017

Phenotypic mechanism of HIV-1 resistance to 3'-azido-3'-deoxythymidine (AZT): increased polymerization processivity and enhanced sensitivity to pyrophosphate of the mutant viral reverse transcriptase

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Unblocking of chain-terminated primer by HIV-1 reverse transcriptase through a nucleotide-dependent mechanism

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Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides

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23 August 2017

The 3'-azido group is not the primary determinant of 3'-azido-3'-deoxythymidine (AZT) responsible for the excision phenotype of AZT-resistant HIV-1.

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23 August 2017

Trapping HIV-1 reverse transcriptase before and after translocation on DNA.

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23 August 2017

Enhanced impairment of chain elongation by inhibitors of HIV reverse transcriptase in cell-free reactions yielding longer DNA products

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14 September 2017

The nucleoside analogs 4'C-methyl thymidine and 4'C-ethyl thymidine block DNA synthesis by wild-type HIV-1 RT and excision proficient NRTI resistant RT variants

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14 September 2017

The K65R reverse transcriptase mutation in HIV-1 reverses the excision phenotype of zidovudine resistance mutations.

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4'-Ethynylstavudine (4'-Ed4T) has potent anti-HIV-1 activity with reduced toxicity and shows a unique activity profile against drug-resistant mutants

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Fixed conformation nucleoside analogs effectively inhibit excision-proficient HIV-1 reverse transcriptases

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A 4'-C-ethynyl-2',3'-dideoxynucleoside analogue highlights the role of the 3'-OH in anti-HIV active 4'-C-ethynyl-2'-deoxy nucleosides

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Delayed chain termination protects the anti-hepatitis B virus drug entecavir from excision by HIV-1 reverse transcriptase

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Selective action of 4'-azidothymidine triphosphate on reverse transcriptase of human immunodeficiency virus type 1 and human DNA polymerases alpha and beta.

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26 June 2018

Metabolism of 4'-azidothymidine. A compound with potent and selective activity against the human immunodeficiency virus

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Broad advances in understanding HIV resistance to antiretrovirals: report on the XVII International HIV Drug Resistance Workshop

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2 September 2018

Opposed steric constraints in human DNA polymerase beta and E. coli DNA polymerase I.

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2 September 2018

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2 September 2018

4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase

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2 September 2018

Structures of HIV-1 RT-DNA complexes before and after incorporation of the anti-AIDS drug tenofovir

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Site-specific footprinting reveals differences in the translocation status of HIV-1 reverse transcriptase. Implications for polymerase translocation and drug resistance.

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2 September 2018

Rapid purification of homodimer and heterodimer HIV-1 reverse transcriptase by metal chelate affinity chromatography.

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2 September 2018

Optimization of parameters for semiempirical methods I. Method

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2'-Deoxy-4'-C-ethynyl-2-fluoroadenosine: a nucleoside reverse transcriptase inhibitor with highly potent activity against all HIV-1 strains, favorable toxic profiles and stability in plasma

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https://pubmed.ncbi.nlm.nih.gov/19837673

12 December 2020

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Nucleotide-induced stable complex formation by HIV-1 reverse transcriptase

1 reference

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12 December 2020

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Separation of Leucocytes: Improved Cell Purity by Fine Adjustments of Gradient Medium Density and Osmolality

1 reference

https://pubmed.ncbi.nlm.nih.gov/19837673

12 December 2020

based on heuristic

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Highly selective action of triphosphate metabolite of 4'-ethynyl D4T: a novel anti-HIV compound against HIV-1 RT

1 reference

https://pubmed.ncbi.nlm.nih.gov/19837673

12 December 2020

based on heuristic

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The generation of hydroxyl radicals in the reaction of molecular oxygen with polyphosphate complexes of ferrous ion

1 reference

https://pubmed.ncbi.nlm.nih.gov/19837673

12 December 2020

based on heuristic

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10.1074/JBC.M109.036616

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10 February 2020

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10 February 2020

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10 February 2020

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