Issue 4, 2016
From the journal:

MedChemComm

De novo design of helical peptides to inhibit tumor necrosis factor-α by disrupting its trimer formation†‡

Qi Shen,§a   Changsheng Zhang,§b   Hongbo Liu,b   Yuting Liu,c   Junyue Cao,d   Xiaolin Zhang,a   Yuan Liang,c   Meiping Zhaoc  and  Luhua Lai*abc  

* Corresponding authors

a Center for Quantitative Biology, Peking University, Beijing 100871, China
E-mail: lhlai@pku.edu.cn

b BNLMS, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, and Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China

c BNLMS, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China

d School of Life Sciences, Peking University, Beijing 100871, China

Abstract

A computational strategy was used to design helical peptides that can bind to tumor necrosis factor-α (TNFα) dimers to prevent active trimer formation. Three designed peptides showed TNFα inhibition at the cellular level. Chemical crosslinking and mass spectrometry studies verified that these peptides function by breaking TNFα trimers.

Graphical abstract: De novo design of helical peptides to inhibit tumor necrosis factor-α by disrupting its trimer formation

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Article information

DOI
https://doi.org/10.1039/C5MD00549C
Article type
Research Article
Submitted
29 Nov 2015
Accepted
21 Jan 2016
First published
22 Jan 2016

Med. Chem. Commun., 2016,7, 725-729

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De novo design of helical peptides to inhibit tumor necrosis factor-α by disrupting its trimer formation

Q. Shen, C. Zhang, H. Liu, Y. Liu, J. Cao, X. Zhang, Y. Liang, M. Zhao and L. Lai, Med. Chem. Commun., 2016, 7, 725 DOI: 10.1039/C5MD00549C

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