Tosedostat

Description: Tosedostat (CHR-2797) is an orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Intracellularly converted into the poorly membrane-permeable active metabolite (CHR-79888), it inhibits puromycin-sensitive aminopeptidase (PuSA) and leukotriene A4 (LTA4) hydrolase. This inhibition in tumor cells may lead to amino acid deprivation, suppressed protein synthesis, increased proapoptotic protein Noxa levels, and ultimately, cell death. Target: Aminopeptidase, AChR. Smiles: CC(C)C[C@H]([C@H](O)C(=O)NO)C(=O)N[C@H](C(=O)OC1CCCC1)c1ccccc1. References: van Herpen CM, et al. Br J Cancer. 2010 Oct 26,103(9):1362-8.