Literature DB >> 18066823

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

Hiroshi Ohrui1, Satoru Kohgo, Hiroyuki Hayakawa, Eiichi Kodama, Masao Matsuoka, Tomohiro Nakata, Hiroaki Mitsuya.   

Abstract

Working hypotheses to solve the critical problems of the existing highly active anti-retroviral therapy were proposed. The study based on the hypotheses proved the validity of the hypotheses and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoroadenosine, a nucleoside reverse transcriptase inhibitor, with highly potent activity against all HIV-1, very favorable toxic profiles, and stability in plasma. The nucleoside will prevent or delay the emergence of drug-resistant HIV-1 variants and be an ideal therapeutic agent for both HIV-1 and HBV infections.

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Year:  2007        PMID: 18066823     DOI: 10.1080/15257770701545218

Source DB:  PubMed          Journal:  Nucleosides Nucleotides Nucleic Acids        ISSN: 1525-7770            Impact factor:   1.381


  14 in total

1.  EFdA, a reverse transcriptase inhibitor, potently blocks HIV-1 ex vivo infection of Langerhans cells within epithelium.

Authors:  Takamitsu Matsuzawa; Tatsuyoshi Kawamura; Youichi Ogawa; Kenji Maeda; Hirotomo Nakata; Kohji Moriishi; Yoshio Koyanagi; Hiroyuki Gatanaga; Shinji Shimada; Hiroaki Mitsuya
Journal:  J Invest Dermatol       Date:  2013-11-11       Impact factor: 8.551

2.  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.

Authors:  Cheryl A Stoddart; Sofiya A Galkina; Pheroze Joshi; Galina Kosikova; Mary E Moreno; Jose M Rivera; Barbara Sloan; Aaron B Reeve; Stefan G Sarafianos; Michael Murphey-Corb; Michael A Parniak
Journal:  Antimicrob Agents Chemother       Date:  2015-05-04       Impact factor: 5.191

3.  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.

Authors:  Yagmur Muftuoglu; Christal D Sohl; Andrea C Mislak; Hiroaki Mitsuya; Stefan G Sarafianos; Karen S Anderson
Journal:  Antiviral Res       Date:  2014-03-12       Impact factor: 5.970

4.  HIV pre-exposure prophylaxis for women and infants prevents vaginal and oral HIV transmission in a preclinical model of HIV infection.

Authors:  Martina Kovarova; Uma Shanmugasundaram; Caroline E Baker; Rae Ann Spagnuolo; Chandrav De; Christopher C Nixon; Angela Wahl; J Victor Garcia
Journal:  J Antimicrob Chemother       Date:  2016-08-01       Impact factor: 5.790

5.  4'-C-methyl-2'-deoxyadenosine and 4'-C-ethyl-2'-deoxyadenosine inhibit HIV-1 replication.

Authors:  B Christie Vu; Paul L Boyer; Maqbool A Siddiqui; Victor E Marquez; Stephen H Hughes
Journal:  Antimicrob Agents Chemother       Date:  2011-02-22       Impact factor: 5.191

6.  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.

Authors:  Christal D Sohl; Kamlendra Singh; Rajesh Kasiviswanathan; William C Copeland; Hiroaki Mitsuya; Stefan G Sarafianos; Karen S Anderson
Journal:  Antimicrob Agents Chemother       Date:  2011-12-12       Impact factor: 5.191

7.  Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine in vitro and in vivo.

Authors:  Michael Murphey-Corb; Premeela Rajakumar; Heather Michael; Julia Nyaundi; Peter J Didier; Aaron B Reeve; Hiroaki Mitsuya; Stefan G Sarafianos; Michael A Parniak
Journal:  Antimicrob Agents Chemother       Date:  2012-06-19       Impact factor: 5.191

8.  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 3 knockout mice.

Authors:  Shinichiro Hattori; Kazuhiko Ide; Hirotomo Nakata; Hideki Harada; Shinya Suzu; Noriyuki Ashida; Satoru Kohgo; Hiroyuki Hayakawa; Hiroaki Mitsuya; Seiji Okada
Journal:  Antimicrob Agents Chemother       Date:  2009-06-22       Impact factor: 5.191

9.  Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA.

Authors:  Eleftherios Michailidis; Emily M Ryan; Atsuko Hachiya; Karen A Kirby; Bruno Marchand; Maxwell D Leslie; Andrew D Huber; Yee T Ong; Jacob C Jackson; Kamalendra Singh; Eiichi N Kodama; Hiroaki Mitsuya; Michael A Parniak; Stefan G Sarafianos
Journal:  Retrovirology       Date:  2013-06-24       Impact factor: 4.602

Review 10.  Current perspectives on HIV-1 antiretroviral drug resistance.

Authors:  Pinar Iyidogan; Karen S Anderson
Journal:  Viruses       Date:  2014-10-24       Impact factor: 5.048

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