| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. <P>SOLUTION: Enzymes having a nucleophilic group at the N-terminus are inhibited as enzyme inhibitors. In some embodiments useful for inhibiting chymotrypsin-like (CT-L) activity of the proteasome, between two and eight backbone units are present, and in some preferred embodiments for CT-L inhibition, between two and six backbone units are present. The side chains extending from the backbone units can include natural aliphatic or aromatic amino acid side chains. In some embodiments, polar or charged residues can be introduced into the peptide epoxides or peptide aziridines. In some embodiments, the backbone units are amide units [-NH-CHR-C(=O)-], in which R is the side chain. <P>COPYRIGHT: (C)2013,JPO&INPIT |
