Exploration of the importance of the P 2-P 3-NHCO-Moiety in a potent di-or tripeptide inhibitor of calpain i: insights into the development of nonpeptidic inhibitors of …
Calpain I, an intracellular cysteine protease, has been implicated in the neurodegeneration following an episode of cerebral ischemia. In this paper, we report on a series of peptidomimetic ketomethylene and carbamethylene inhibitors of recombinant human calpain I (rh calpain I). Our study reveals that the-NHCO-moiety (possible hydrogen-bonding site) at the P2-P3 region of a potent tripeptide or a dipeptide inhibitor of calpain I is not a ...