Peptide Inhibitors of IKB Protease: Modification of the C-termini of Z-LLF-CHO

MJ Suto, RW Sullivan, LJ Ransone

Index: Suto, Mark J.; Sullivan, Robert W.; Ransone, Lynn J. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 24 p. 2925 - 2930

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Citation Number: 7

Abstract

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-κB through inhibition of IκB protease. Of the compounds evaluated only the C-terminal aldehydes 5a, b were active in our Jurkat T-cell based assay. Compound 5a also decreased IL-2 and IL-8 levels in these cells indicating that inhibitors of IκB protease can have an effect on various ...