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aminopeptidase inhibitor CHR-2797 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. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
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Code name: | ![](https://webarchive.library.unt.edu/eot2008/20081005072736im_/http://www.nci.nih.gov/images/spacer.gif) | CHR-2797 | | ![](https://webarchive.library.unt.edu/eot2008/20081005072736im_/http://www.nci.nih.gov/images/spacer.gif) |
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