Literature DB >> 17150787

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.

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

Abstract

A working hypothesis to solve the critical problems of existing HAART was proposed. The study based on the hypothesis proved the validity of the hypothesis and resulted in the development of 2'-deoxy-4'-C-ethynyl-2-fluoro-adenosine (4'Ed2FA), a nucleoside reverse transcriptase inhibitor (NRTI) with highly potent activity against all HIV-1 strains, very favourable toxic profiles, and stability in plasma.

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Year:  2006        PMID： 17150787     DOI： 10.1093/nass/nrl001

Source DB:  PubMed          Journal:  Nucleic Acids Symp Ser (Oxf)        ISSN： 0261-3166


  8 in total

Review 1.  Emerging reverse transcriptase inhibitors for HIV-1 infection.

Authors:  Mohammad A Rai; Sam Pannek; Carl J Fichtenbaum
Journal:  Expert Opin Emerg Drugs       Date:  2018-05-10       Impact factor: 4.191

2.  Effect of translocation defective reverse transcriptase inhibitors on the activity of N348I, a connection subdomain drug resistant HIV-1 reverse transcriptase mutant.

Authors:  E Michailidis; K Singh; E M Ryan; A Hachiya; Y T Ong; K A Kirby; B Marchand; E N Kodama; H Mitsuya; M A Parniak; S G Sarafianos
Journal:  Cell Mol Biol (Noisy-le-grand)       Date:  2012-12-22       Impact factor: 1.770

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

Authors:  Vincent H Wu; Robert A Smith; Sara Masoum; Dana N Raugi; Selly Ba; Moussa Seydi; Jay A Grobler; Geoffrey S Gottlieb
Journal:  Antimicrob Agents Chemother       Date:  2017-07-25       Impact factor: 5.191

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

Authors:  Eleftherios Michailidis; Bruno Marchand; Eiichi N Kodama; Kamlendra Singh; Masao Matsuoka; Karen A Kirby; Emily M Ryan; Ali M Sawani; Eva Nagy; Noriyuki Ashida; Hiroaki Mitsuya; Michael A Parniak; Stefan G Sarafianos
Journal:  J Biol Chem       Date:  2009-12-18       Impact factor: 5.157

Review 5.  4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor.

Authors:  Martin Markowitz; Stefan G Sarafianos
Journal:  Curr Opin HIV AIDS       Date:  2018-07       Impact factor: 4.283

Review 6.  Structure and function of HIV-1 reverse transcriptase: molecular mechanisms of polymerization and inhibition.

Authors:  Stefan G Sarafianos; Bruno Marchand; Kalyan Das; Daniel M Himmel; Michael A Parniak; Stephen H Hughes; Eddy Arnold
Journal:  J Mol Biol       Date:  2008-11-03       Impact factor: 5.469

7.  Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.

Authors:  Tomas Cihlar; Adrian S Ray; Constantine G Boojamra; Lijun Zhang; Hon Hui; Genevieve Laflamme; Jennifer E Vela; Deborah Grant; James Chen; Florence Myrick; Kirsten L White; Ying Gao; Kuei-Ying Lin; Janet L Douglas; Neil T Parkin; Anne Carey; Rowchanak Pakdaman; Richard L Mackman
Journal:  Antimicrob Agents Chemother       Date:  2007-12-03       Impact factor: 5.191

8.  Antiviral Drug Discovery To Address the COVID-19 Pandemic.

Authors:  Douglas D Richman
Journal:  mBio       Date:  2020-09-25       Impact factor: 7.867
  8 in total

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