Acetyl-pepstatin ammonium is an aspartic protease ( PRs ) inhibitor that targets HIV-1 protease and XMRV protease with K i values of 13 nM and 712 nM, respectively. Acetyl-pepstatin ammonium inhibits XMRV protease by blocking cleavage through mixed-mode binding. Acetyl-pepstatin ammonium can be used in research related to HIV-1 and XMRV infection [1].
In Vitro, Acetyl-pepstatin (1 h) ammonium inhibits recombinant XMRV PR in an HPLC-based protease assay with an apparent Ki of 712 nM, and inhibits recombinant HIV-1 PR with an apparent Ki of 13 nM[1]. Acetyl-pepstatin (3.0 μM; 1 h) ammonium produces 50% inhibition of XMRV PR-mediated cleavage of recombinant MLV Gag fragments in SDS-PAGE experiments[1]. Acetyl-pepstatin ammonium binds XMRV PR in a mixed mode, involving two half-occupied head-to-head molecules and one half-occupied standard-mode molecule, as determined by the 2.0 Å crystal structure PDB 4EXH[1].
References:
[1]. Matúz K, et al. Inhibition of XMRV and HIV-1 proteases by pepstatin A and acetyl-pepstatin. The FEBS journal. 2012 Sep;279(17):3276-86.
In Vitro, Acetyl-pepstatin (1 h) ammonium inhibits recombinant XMRV PR in an HPLC-based protease assay with an apparent Ki of 712 nM, and inhibits recombinant HIV-1 PR with an apparent Ki of 13 nM[1]. Acetyl-pepstatin (3.0 μM; 1 h) ammonium produces 50% inhibition of XMRV PR-mediated cleavage of recombinant MLV Gag fragments in SDS-PAGE experiments[1]. Acetyl-pepstatin ammonium binds XMRV PR in a mixed mode, involving two half-occupied head-to-head molecules and one half-occupied standard-mode molecule, as determined by the 2.0 Å crystal structure PDB 4EXH[1].
References:
[1]. Matúz K, et al. Inhibition of XMRV and HIV-1 proteases by pepstatin A and acetyl-pepstatin. The FEBS journal. 2012 Sep;279(17):3276-86.