EFdA-TP tetraammonium 是一种有效的核苷逆转录酶 (RT) 抑制剂。EFdA-TP tetraammonium 作为有效的立即或延迟链终止剂 (ICT 或 DCT) 抑制 RT 催化的 DNA 合成。EFdA-TP tetraammonium 通过多种机制抑制 HIV-1 RT。
EFdA-TP tetraammonium is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP tetraammonium inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP tetraammonium inhibits HIV-1 RT with multiple mechanisms[1].
EFdA-TP tetraammonium (0.05-10 μM; for 15 min) inhibits RT-catalyzed DNA synthesis as an ICT or DCT[1]. EFdA-TP tetraammonium can block RT as a translocation-defective RT inhibitor that dramatically slows DNA synthesis, acting as a de facto immediate chain terminator. EFdA-TP tetraammonium can function as a delayed chain terminator, allowing incorporation of an additional dNTP before blocking DNA synthesis[1].
[1]. Martin Markowitz, et al. 4’-Ethynyl-2-fluoro-2’-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor. Curr Opin HIV AIDS. 2018 Jul;13(4):294-299.
[2]. Eleftherios Michailidis, et al. 4’-Ethynyl-2-fluoro-2’-deoxyadenosine (EFdA) inhibits HIV-1 reverse transcriptase with multiple mechanisms. J Biol Chem. 2014 Aug 29;289(35):24533-48.
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