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

作者：Feng, Zhaoqianqi; Wang, Huaimin; Du, Xuewen; Shi, Junfeng; Li, Jie; Xu, Bing^*

来源：Chemical communications, 2016, 52(37): 6332-6335.

DOI：10.1039/c6cc02282k

• PRION-LIKE NANOFIBRILS
• SMALL MOLECULES PRISM
• ALKALINE-PHOSPHATASE
• SUPRAMOLECULAR HYDROGELS
• RATIONAL DESIGN
• DEATH
• INHIBITION
• DYNAMICS
• FATE

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 mu M) towards an osteosarcoma cell line.

• 出版日期2016