4′-Ethynyl-2-fluoro-2′-deoxyadenosine, MK-8591
نویسندگان
چکیده
منابع مشابه
Structural basis of HIV inhibition by translocation-defective RT inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA).
4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) is the most potent nucleoside analog inhibitor of HIV reverse transcriptase (RT). It retains a 3'-OH yet acts as a chain-terminating agent by diminishing translocation from the pretranslocation nucleotide-binding site (N site) to the posttranslocation primer-binding site (P site). Also, facile misincorporation of EFdA-monophosphate (MP) results in di...
متن کاملDelayed emergence of HIV-1 variants resistant to 4'-ethynyl-2-fluoro-2'-deoxyadenosine: comparative sequential passage study with lamivudine, tenofovir, emtricitabine and BMS-986001.
BACKGROUND 4'-Ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) contains an ethynyl moiety and the 3'-hydroxyl and exerts highly potent activity against various HIV type-1 (HIV-1) strains including multi-drug-resistant variants. METHODS Comparative selection passages against EFdA, lamivudine (3TC), tenofovir disoproxil fumarate (TDF), emtricitabine (FTC) or BMS-986001 (Ed4T) were conducted using a mi...
متن کاملMechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor.
Nucleoside reverse transcriptase inhibitors (NRTIs) are employed in first line therapies for the treatment of human immunodeficiency virus (HIV) infection. They generally lack a 3'-hydroxyl group, and thus when incorporated into the nascent DNA they prevent further elongation. In this report we show that 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA), a nucleoside analog that retains a 3'-hydroxy...
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The title compound, C(8)H(7)FO(2), crystallizes as discrete mol-ecules, the conformation of which may be influenced by an intra-molecular hydr-oxy-carbonyl O-H⋯O hydrogen bond.
متن کامل2-(2-Fluoro-4-nitrophenoxy)-3-nitropyridine
In the title compound, C11H6FN3O5, the dihedral angle between the aromatic rings is 72.4 (3)°. The NO2 groups form dihedral angles of 40.8 (2) and 4.8 (2)°, respectively, with the attached pyridine and benzene rings. The crystal structure features π-π stacking between centrosymmetrically related pairs of pyridine rings [centroid-centroid separation = 3.800 (3) Å].
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ژورنال
عنوان ژورنال: Current Opinion in HIV and AIDS
سال: 2018
ISSN: 1746-630X
DOI: 10.1097/coh.0000000000000467