M
Michael A. Parniak
Researcher at University of Pittsburgh
Publications - 96
Citations - 4079
Michael A. Parniak is an academic researcher from University of Pittsburgh. The author has contributed to research in topics: Reverse transcriptase & RNase H. The author has an hindex of 34, co-authored 96 publications receiving 3752 citations. Previous affiliations of Michael A. Parniak include McGill University & Center for Advanced Biotechnology and Medicine.
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Journal ArticleDOI
Structure and function of HIV-1 reverse transcriptase: molecular mechanisms of polymerization and inhibition.
Stefan G. Sarafianos,Bruno Marchand,Kalyan Das,Daniel M. Himmel,Michael A. Parniak,Stephen H. Hughes,Edward Arnold +6 more
TL;DR: A better understanding of the structure and function of RT and of the mechanism(s) of inhibition can be used to generate better drugs; in particular, drugs that are effective against the current drug-resistant strains of HIV-1.
Journal ArticleDOI
Selective inhibition of HIV-1 reverse transcriptase-associated ribonuclease H activity by hydroxylated tropolones
Scott R. Budihas,Inna Gorshkova,Sergei Gaidamakov,Antony Wamiru,Marion K. Bona,Michael A. Parniak,Robert J. Crouch,James B. McMahon,John A. Beutler,Stuart F. J. Le Grice +9 more
TL;DR: β-thujaplicinol and manicol failed to inhibit DNA-dependent DNA polymerase activity of HIV-1 RT at a concentration of 50 μM, suggesting that they are specific for the C-terminal RNase H domain, while surface plasmon resonance studies indicated that the inhibition was not due to intercalation of the analog into the nucleic acid substrate.
Journal ArticleDOI
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site.
Daniel M. Himmel,Stefan G. Sarafianos,Stefan G. Sarafianos,Sanjeewa Dharmasena,Mohammed M. Hossain,Kessler McCoy-Simandle,Tatiana V Ilina,Arthur D. Clark,Jennifer L. Knight,John G. Julias,Patrick K. Clark,Karsten Krogh-Jespersen,Ronald M. Levy,Stephen H. Hughes,Michael A. Parniak,Eddy Arnold +15 more
TL;DR: Sub substituted DHBNH derivatives that interact with the NNRTI-binding pocket inhibit both the polymerase and RNH activities of RT and inhibit the initiation of RNA-primed DNA synthesis.
Journal ArticleDOI
A fluorescence-based high-throughput screening assay for inhibitors of human immunodeficiency virus-1 reverse transcriptase-associated ribonuclease H activity.
TL;DR: A fluorescence resonance energy transfer assay readily applicable to 96-well and 384-well microplate formats with robotic operation was developed to enable high-throughput screening for inhibitors of human immunodeficiency virus-1 (HIV-1) reverse transcriptase (RT)-associated RNase H activity, an underexplored target for antiretroviral development.
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Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor
Eleftherios Michailidis,Bruno Marchand,Eiichi Kodama,Kamlendra Singh,Masao Matsuoka,Karen A. Kirby,Emily M. Ryan,Ali M. Sawani,Eva Nagy,Noriyuki Ashida,Hiroaki Mitsuya,Hiroaki Mitsuya,Michael A. Parniak,Stefan G. Sarafianos +13 more
TL;DR: 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA), a nucleoside analog that retains a 3′-hydroxyl moiety, inhibited HIV-1 replication in activated peripheral blood mononuclear cells with an EC50 of 0.05 nm, a potency several orders of magnitude better than any of the current clinically used NRTIs.