Author/Authors :
Sankar Chatterjee، نويسنده , , Kurt Josef، نويسنده , , Gregory Wells، نويسنده , , Mohamed Iqbal، نويسنده , , Ron Bihovsky، نويسنده , , John P. Mallamo، نويسنده , , Mark A. Ator، نويسنده , , Donna Bozyczko-Coyne، نويسنده , , Satish Mallya، نويسنده , , Shobha Senadhi، نويسنده , , Robert Siman، نويسنده ,
Abstract :
We report on a series of potent and selective dipeptide fluoromethyl ketone inhibitors of recombinant human calpain I. Compound 4f, having a tetrahydroisoquinoline containing urea motif as N-terminus capping group, is the most potent member (kobs/I = 276,000 M−1 s−1) of this class. This compound was shown to prefer calpain I by >36-fold and approximately 4-fold over the related cysteine proteases, cathepsin B and cathepsin L, respectively.
