Literature DB >> 28559249

MK-8591 (4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture.

Vincent H Wu1, Robert A Smith2, Sara Masoum1, Dana N Raugi1, Selly Ba3, Moussa Seydi3, Jay A Grobler4, Geoffrey S Gottlieb1,5.   

Abstract

There is a pressing need to identify more effective antiretroviral drugs for HIV-2 treatment. Here, we show that the investigational compound MK-8591 (4'-ethynyl-2-fluoro-2'-deoxyadenosine [EFdA]) is highly active against group A and B isolates of HIV-2; 50% effective concentrations [EC50] for HIV-2 were, on average, 4.8-fold lower than those observed for HIV-1. MK-8591 also retains potent activity against multinucleoside-resistant HIV-2 mutants (EC50 ≤ 11 nM). These data suggest that MK-8591 may have antiviral activity in HIV-2-infected individuals.
Copyright © 2017 American Society for Microbiology.

Entities:  

Keywords:  4′-ethynyl-2-fluoro-2′-deoxyadenosine; EFdA; HIV-1; HIV-2; MK-8591; NRTI; antiretroviral therapy; drug resistance

Mesh：

Substances：

Year:  2017        PMID： 28559249      PMCID： PMC5527656          DOI： 10.1128/AAC.00744-17

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  54 in total

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Authors:  Robert A Smith; Dana N Raugi; Vincent H Wu; Sally S Leong; Kate M Parker; Mariah K Oakes; Papa Salif Sow; Selly Ba; Moussa Seydi; Geoffrey S Gottlieb
Journal:  Antimicrob Agents Chemother       Date:  2015-09-21       Impact factor: 5.191

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Authors:  Ana Treviño; Carmen de Mendoza; Estrella Caballero; Carmen Rodríguez; Patricia Parra; Rafael Benito; Teresa Cabezas; Lourdes Roc; Antonio Aguilera; Vincent Soriano
Journal:  J Antimicrob Chemother       Date:  2011-05-10       Impact factor: 5.790

6.  Letter. In vitro phenotypic susceptibility to nucleoside reverse transcriptase inhibitors of HIV-2 isolates with the Q151M mutation in the reverse transcriptase gene.

Authors:  Florence Damond; Gilles Collin; Sophie Matheron; Gilles Peytavin; Pauline Campa; Séverine Delarue; Audrey Taieb; Antoine Bénard; Geneviève Chêne; Françoise Brun-Vézinet; Diane Descamps
Journal:  Antivir Ther       Date:  2005

7.  Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides.

Authors:  R F Schinazi; R M Lloyd; M H Nguyen; D L Cannon; A McMillan; N Ilksoy; C K Chu; D C Liotta; H Z Bazmi; J W Mellors
Journal:  Antimicrob Agents Chemother       Date:  1993-04       Impact factor: 5.191

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Authors:  Thushan I de Silva; Matthew Cotten; Sarah L Rowland-Jones
Journal:  Trends Microbiol       Date:  2008-10-27       Impact factor: 17.079
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Authors:  Robert A Smith; Dana N Raugi; Vincent H Wu; Christopher G Zavala; Jennifer Song; Khardiata Mbaye Diallo; Moussa Seydi; Geoffrey S Gottlieb
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Authors:  Shalley N Kudalkar; Jagadish Beloor; Elias Quijano; Krasimir A Spasov; Won-Gil Lee; José A Cisneros; W Mark Saltzman; Priti Kumar; William L Jorgensen; Karen S Anderson
Journal:  Proc Natl Acad Sci U S A       Date:  2017-12-26       Impact factor: 11.205

4.  The High Genetic Barrier of EFdA/MK-8591 Stems from Strong Interactions with the Active Site of Drug-Resistant HIV-1 Reverse Transcriptase.

Authors:  Yuki Takamatsu; Debananda Das; Satoru Kohgo; Hironori Hayashi; Nicole S Delino; Stefan G Sarafianos; Hiroaki Mitsuya; Kenji Maeda
Journal:  Cell Chem Biol       Date:  2018-08-30       Impact factor: 8.116

5.  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.

Authors:  Maria E Cilento; Aaron B Reeve; Eleftherios Michailidis; Tatiana V Ilina; Eva Nagy; Hiroaki Mitsuya; Michael A Parniak; Philip R Tedbury; Stefan G Sarafianos
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6.  In Vitro Antiviral Activity of Cabotegravir against HIV-2.

Authors:  Robert A Smith; Vincent H Wu; Christopher G Zavala; Dana N Raugi; Selly Ba; Moussa Seydi; Geoffrey S Gottlieb
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7.  Long-acting implants to treat and prevent HIV infection.

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Review 8.  Approved HIV reverse transcriptase inhibitors in the past decade.

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