PEPTIDE INHIBITORS OF I-KAPPA-B PROTEASE - MODIFICATION OF THE C-TERMINI OF Z-LLF-CHO

A series of tripeptides (Z-LLF-R) with various modifications at their C-terminus were synthesized and evaluated for their ability to prevent the activation of NF-kappa B through inhibition of I kappa B protease . Of the compounds evaluated only the C-terminal aldehydes 5a,b were a ctive in our Jurkat T-cell based assay. Compound 5a also decreased IL- 2 and IL-8 levels in these cells indicating that inhibitors of I kappa B protease can have an effect on various signaling pathways. Copyrigh t (C) 1996 Elsevier Science Ltd