Minimal C-terminal modification boosts peptide self-assembling ability for necroptosis of cancer cells

Abstract

Here we reported the first case in which enhancing self-assembling ability boosts anti-cancer efficacy through a simple and minimal modification of the C-terminus of a D-tripeptide. By only a 2% change of the molecular weight, this facile approach increases the inhibitory activity by over an order of magnitude (IC₅₀ from 431 to 23 μM) towards an osteosarcoma cell line.