Bioorganic and Medicinal Chemistry Letters p. 2925 - 2930 (1996)
Update date:2022-09-26
Topics:
Suto, Mark J.
Sullivan, Robert W.
Ransone, Lynn J.
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. Compounds 5a also decreased IL-2 and IL-8 levels in these cells indicating that inhibitors of IκB protease can have an effect on various signalling pathways.
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