Small-molecule inhibitor: MLN-4760

Name

History: MLN-4760 was first described as compound 15 by Dales et al. (2002) who write 'We conceived nonhydrolyzable His-Leu-like molecules bearing a C-terminal carboxylate and including a centrally located carboxylate to serve as a zinc coordinating element. We chose the carboxylate as the zinc binding fragment on the basis of precedence with a known carboxypeptidase A inhibitor, benzylsuccinic acid.'
Peptidases inhibited: Angiotensin-converting enzyme-2 (Dales et al., 2002).
Mechanism: This is a reversible, picomolar inhibitor of angiotensin-converting enzyme-2 (Dales et al., 2002). The structure of the complex has been solved (Towler et al., 2004).

CID at PubChem: 448281
Structure
Chemical/biochemical name: (S,S)-2-[1-carboxy-2-[3-(3,5-dichlorobenzyl)-3H-imidazol4-yl]-ethylamino]-4-methylpentanoic acid
Formula weight: 428