Issue 7, 2016

Systematic network-based discovery of a Fam20C inhibitor (FL-1607) with apoptosis modulation in triple-negative breast cancer

Abstract

Family with sequence similarity 20, member C (Fam20C) is a physiological Golgi casein kinase that phosphorylates multiple secreted proteins. Recently, it has been reported that Fam20C can be identified as a novel kinase target for therapeutic development. Thus, inhibition of Fam20C will be a potential therapeutic strategy to prevent tumor cell progression and metastasis. In our study, based upon the systems-biology network, molecular modeling and molecular dynamics (MD) simulations, we discovered a novel Fam20C inhibitor (FL-1607) with potent anti-proliferative effects on triple-negative breast cancer (TNBC) cells. Subsequently, we found that this Fam20C inhibitor could induce apoptosis and inhibit cell migration in MDA-MB-468 cells. Together, these findings would provide a new clue to the exploration of more novel Fam20C inhibitors for future TNBC therapy.

Graphical abstract: Systematic network-based discovery of a Fam20C inhibitor (FL-1607) with apoptosis modulation in triple-negative breast cancer

Supplementary files

Article information

Article type
Paper
Submitted
11 Cʼhwe. 2016
Accepted
06 Ebr. 2016
First published
26 Ebr. 2016

Mol. BioSyst., 2016,12, 2108-2118

Systematic network-based discovery of a Fam20C inhibitor (FL-1607) with apoptosis modulation in triple-negative breast cancer

Z. Qin, P. Wang, X. Li, S. Zhang, M. Tian, Y. Dai and L. Fu, Mol. BioSyst., 2016, 12, 2108 DOI: 10.1039/C6MB00111D

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