Structural basis of HIV inhibition by translocation-defective RT inhibitor 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA)

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA)

Significance 4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA), a potent antiviral with an unusually long half-life, is currently in phase I clinical trials. It inhibits reverse transcriptase (RT) through a mechanism of action different from all approved anti-HIV drugs: After incorporation in the nascent...

Szczegółowa specyfikacja

Zapisane w:

Opis bibliograficzny
Główni autorzy:	Zhe Salie, Karen A. Kirby, Eleftherios Michailidis, Bruno Marchand, Kamalendra Singh, Lisa C. Rohan, Eiichi Kodama, Hiroaki Mitsuya, Michael A. Parniak, Stefan G. Sarafianos
Format:	Artigo
Język:	angielski
Wydane:	2016
Dostęp online:	https://doi.org/10.1073/pnas.1605223113 https://www.pnas.org/content/pnas/113/33/9274.full.pdf
Etykiety:	Dodaj etykietę Nie ma etykietki, Dołącz pierwszą etykiete!

Podobne zapisy

Structural basis of HIV inhibition by translocation-defective RT inhibitor 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA)
od: Salie, Zhe Li, i wsp.
Wydane: (2016)

4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) Inhibits HIV-1 Reverse Transcriptase with Multiple Mechanisms
od: Eleftherios Michailidis, i wsp.
Wydane: (2014)

4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) Inhibits HIV-1 Reverse Transcriptase with Multiple Mechanisms
od: Michailidis, Eleftherios, i wsp.
Wydane: (2014)

Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA
od: Michailidis, Eleftherios, i wsp.
Wydane: (2013)

EFdA (4′-ethynyl-2-fluoro-2′-deoxyadenosine, MK-8591): A Novel HIV-1 Reverse Transcriptase Translocation Inhibitor
od: Markowitz, Martin, i wsp.
Wydane: (2018)

Effects of Substitutions at the 4′ and 2 Positions on the Bioactivity of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine
od: Kirby, Karen A., i wsp.
Wydane: (2013)

Probing the molecular mechanism of action of the HIV-1 reverse transcriptase inhibitor 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) using pre-steady-state kinetics
od: Muftuoglu, Yagmur, i wsp.
Wydane: (2014)

Evaluation of Combinations of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine with Clinically Used Antiretroviral Drugs
od: Hachiya, Atsuko, i wsp.
Wydane: (2013)

Oral Administration of the Nucleoside EFdA (4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine) Provides Rapid Suppression of HIV Viremia in Humanized Mice and Favorable Pharmacokinetic Properties in Mice and the Rhesus Macaque
od: Stoddart, Cheryl A., i wsp.
Wydane: (2015)

Oral Administration of the Nucleoside EFdA (4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine) Provides Rapid Suppression of HIV Viremia in Humanized Mice and Favorable Pharmacokinetic Properties in Mice and the Rhesus Macaque
od: Cheryl A. Stoddart, i wsp.
Wydane: (2015)

Cellular HIV Reservoirs and Viral Rebound from the Lymphoid Compartments of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine (EFdA)-Suppressed Humanized Mice
od: Maidji, Ekaterina, i wsp.
Wydane: (2019)

THE SUGAR RING CONFORMATION OF 4’-ETHYNYL-2-FLUORO-2’-DEOXYADENOSINE AND ITS RECOGNITION BY THE POLYMERASE ACTIVE SITE OF HIV REVERSE TRANSCRIPTASE
od: Kirby, K.A., i wsp.
Wydane: (2011)

Mechanism of Inhibition of HIV-1 Reverse Transcriptase by 4′-Ethynyl-2-fluoro-2′-deoxyadenosine Triphosphate, a Translocation-defective Reverse Transcriptase Inhibitor
od: Eleftherios Michailidis, i wsp.
Wydane: (2009)

Mechanism of Inhibition of HIV-1 Reverse Transcriptase by 4′-Ethynyl-2-fluoro-2′-deoxyadenosine Triphosphate, a Translocation-defective Reverse Transcriptase Inhibitor
od: Michailidis, Eleftherios, i wsp.
Wydane: (2009)

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention
od: Zhang, Wei, i wsp.
Wydane: (2013)

4′-Ethynyl-2-fluoro-2′-deoxyadenosine, MK-8591
od: Martin Markowitz, i wsp.
Wydane: (2018)

Development of Human Immunodeficiency Virus Type 1 Resistance to 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine Starting with Wild-Type or Nucleoside Reverse Transcriptase Inhibitor-Resistant Strains
od: Cilento, Maria E., i wsp.
Wydane: (2021)

In vitro transport characteristics of EFdA, a novel nucleoside reverse transcriptase inhibitor using Caco-2 and MDCKII cell monolayers
od: Zhang, Wei, i wsp.
Wydane: (2014)

Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor
od: Zhang, Wei, i wsp.
Wydane: (2013)

Vaginal microbicide film combinations of two reverse transcriptase inhibitors, EFdA and CSIC, for the prevention of HIV-1 sexual transmission
od: Zhang, Wei, i wsp.
Wydane: (2015)

Response of Simian Immunodeficiency Virus to the Novel Nucleoside Reverse Transcriptase Inhibitor 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine In Vitro and In Vivo
od: Murphey-Corb, Michael, i wsp.
Wydane: (2012)

Vaginal Microbicide Film Combinations of Two Reverse Transcriptase Inhibitors, EFdA and CSIC, for the Prevention of HIV-1 Sexual Transmission
od: Wei Zhang, i wsp.
Wydane: (2015)

Efficient Inhibition of HIV Replication in the Gastrointestinal and Female Reproductive Tracts of Humanized BLT Mice by EFdA
od: Shanmugasundaram, Uma, i wsp.
Wydane: (2016)

Response of Simian Immunodeficiency Virus to the Novel Nucleoside Reverse Transcriptase Inhibitor 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine <i>In Vitro</i> and <i>In Vivo</i>
od: Michael Murphey‐Corb, i wsp.
Wydane: (2012)

The high genetic barrier of EFdA/MK-8591 stems from strong interactions with the active site of drug-resistant HIV-1 reverse transcriptase
od: Takamatsu, Yuki, i wsp.
Wydane: (2018)

Activity against Human Immunodeficiency Virus Type 1, Intracellular Metabolism, and Effects on Human DNA Polymerases of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine
od: Nakata, Hirotomo, i wsp.
Wydane: (2007)

Activity against Human Immunodeficiency Virus Type 1, Intracellular Metabolism, and Effects on Human DNA Polymerases of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine
od: Hirotomo Nakata, i wsp.
Wydane: (2007)

Mechanism of Interaction of Human Mitochondrial DNA Polymerase γ with the Novel Nucleoside Reverse Transcriptase Inhibitor 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine Indicates a Low Potential for Host Toxicity
od: Sohl, Christal D., i wsp.
Wydane: (2012)

EFdA, a Reverse Transcriptase Inhibitor, Potently Blocks HIV-1 Ex Vivo Infection of Langerhans Cells within Epithelium
od: Matsuzawa, Takamitsu, i wsp.
Wydane: (2013)

Antiretroviral potency of 4′-ethnyl-2′-fluoro-2′-deoxyadenosine, tenofovir alafenamide and second-generation NNRTIs across diverse HIV-1 subtypes
od: Njenda, Duncan T, i wsp.
Wydane: (2018)

Structural Aspects of Drug Resistance and Inhibition of HIV-1 Reverse Transcriptase
od: Singh, Kamalendra, i wsp.
Wydane: (2010)

Structural Aspects of Drug Resistance and Inhibition of HIV-1 Reverse Transcriptase
od: Kamalendra Singh, i wsp.
Wydane: (2010)

HIV-1 Reverse Transcriptase (RT) Polymorphism 172K Suppresses the Effect of Clinically Relevant Drug Resistance Mutations to Both Nucleoside and Non-nucleoside RT Inhibitors
od: Hachiya, Atsuko, i wsp.
Wydane: (2012)

MK-8591 (4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture
od: Wu, Vincent H., i wsp.
Wydane: (2017)

K70Q Adds High-Level Tenofovir Resistance to “Q151M Complex” HIV Reverse Transcriptase through the Enhanced Discrimination Mechanism
od: Hachiya, Atsuko, i wsp.
Wydane: (2011)

M184I/V substitutions and E138K/M184I/V double substitutions in HIV reverse transcriptase do not significantly affect the antiviral activity of EFdA
od: Oliveira, Maureen, i wsp.
Wydane: (2017)

MtEFD and MtEFD2: Two transcription factors with distinct neofunctionalization in symbiotic nodule development
od: Jardinaud, Marie-Françoise, i wsp.
Wydane: (2022)

The N348I Mutation at the Connection Subdomain of HIV-1 Reverse Transcriptase Decreases Binding to Nevirapine
od: Schuckmann, Matthew M., i wsp.
Wydane: (2010)

EFFECT OF TRANSLOCATION DEFECTIVE REVERSE TRANSCRIPTASE INHIBITORS ON THE ACTIVITY OF N348I, A CONNECTION SUBDOMAIN DRUG RESISTANT HIV-1 REVERSE TRANSCRIPTASE MUTANT
od: MICHAILIDIS, E., i wsp.
Wydane: (2012)

4′-Ethynyl Nucleoside Analogs: Potent Inhibitors of Multidrug-Resistant Human Immunodeficiency Virus Variants In Vitro
od: Eiichi Kodama, i wsp.
Wydane: (2001)