NCIt definition : A proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with
potential antineoplastic activity. Aminopeptidase inhibitor CHR-2797 is converted
intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which
inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase
(PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in
tumor cells may result in amino acid deprivation, inhibition of protein synthesis
due to a decrease in the intracellular free amino acid pool, an increase in the level
of the proapoptotic protein Noxa, and cell death. Noxa is a member of the BH3 (Bcl-2
homology 3)-only subgroup of the proapoptotic Bcl-2 (B-cell CLL/lymphoma 2) protein
family.;