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 …

…, TM O'Kane, BA McKenna, D Bozyczko-Coyne…

Index: Chatterjee; Iqbal; Mallya; Senadhi; O'Kane; McKenna; Bozyczko-Coyne; Kauer; Siman; Mallamo Bioorganic and medicinal chemistry, 1998 , vol. 6, # 5 p. 509 - 522

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Citation Number: 17

Abstract

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 ...