Uses
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle[1][2]. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
Biological Activity
PF74 (PF-3450074) is a HIV-1 inhibitor th at targets HIV capsid protein. PF74 binds specifically to HIV-1 particles and triggers premature HIV-1 uncoating in target cells.
IC 50
HIV-1 (NL4.3 strain): 0.72 μM (IC
50)
References
[1] Xu JP, et al. Exploring?Modifications?of an?HIV-1?Capsid?Inhibitor:?Design,?Synthesis, and?Mechanism?of?Action.J Drug Des Res.?2018;5(2). pii: 1070. Epub 2018 Aug 13. PMID:30393786
[2] Shi J, et al. Small-molecule inhibition of human immunodeficiency virus type 1 infection by virus capsid destabilization.J Virol. 2011 Jan;85(1):542-9. DOI:
10.1128/JVI.01406-10
