EFdA-TP

Names

[ Name ]:
EFdA-TP

Biological Activity

[Description]:

EFdA-TP is a potent nucleoside reverse transcriptase (RT) inhibitor. EFdA-TP inhibits RT-catalyzed DNA synthesis as an effective immediate or delayed chain terminator (ICT or DCT). EFdA-TP inhibits HIV-1 RT with multiple mechanisms[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Signaling Pathways >> Anti-infection >> Reverse Transcriptase

[Target]

HIV-1

[In Vitro]

EFdA-TP (0.05-10 μM; for 15 min) inhibits RT-catalyzed DNA synthesis as an ICT or DCT[1]. EFdA-TP can block RT as a translocation-defective RT inhibitor that dramatically slows DNA synthesis, acting as a de facto immediate chain terminator. EFdA-TP can function as a delayed chain terminator, allowing incorporation of an additional dNTP before blocking DNA synthesis[1].

[References]

[1]. 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.

[2]. 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₂H₁₅FN₅O₁₂P₃

[ Molecular Weight ]:
533.19

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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