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Chemical Compound Review

AC1OCCUU     (2S,4S,5S)-6-cyclohexyl-5- (3,3...

Synonyms: U-81749, U-81749E, U 81749, 126103-94-4, TBA-CVA-Ile-Amp, ...
 
 
 
 
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Disease relevance of U-81749

  • The peptide U-81749 inhibited recombinant HIV-1 protease in vitro (inhibition constant Ki of 70 nanomolar) and HIV-1 replication in human peripheral blood lymphocytes (inhibitory concentration IC50 of 0.1 to 1 micromolar) [1].
  • Moreover, 10 micromolar concentrations of U-81749 significantly inhibited proteolysis of the HIV-1 gag polyprotein (p55) to the mature viral structural proteins p24 and p17 in cells infected with a recombinant vaccinia virus expressing the HIV-1 gag-pol genes [1].

References

  1. A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation. McQuade, T.J., Tomasselli, A.G., Liu, L., Karacostas, V., Moss, B., Sawyer, T.K., Heinrikson, R.L., Tarpley, W.G. Science (1990) [Pubmed]
 
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