Issue 6, 2015

Retracted Article: Identifying the inhibitory mechanism of apigenin on the insulin ligand–receptor binding

Abstract

Although apigenin, a plant flavone, has been shown to inhibit the activation of insulin receptor signaling, its inhibitory mechanism is largely unknown. In this work, using single-molecule force measurement and fluorescence imaging, we demonstrate that apigenin inhibits insulin-induced dimerization of the insulin receptor (IR) through blocking ligand–receptor interactions. This inhibitory effect is also confirmed by flow cytometry and molecular docking. Furthermore we show that apigenin impairs cancer cell proliferation. The role of apigenin in suppressing tumor growth was also evident in an in vivo model, indicating a potential future application of apigenin in cancer therapy.

Graphical abstract: Retracted Article: Identifying the inhibitory mechanism of apigenin on the insulin ligand–receptor binding

Associated articles

Supplementary files

Article information

Article type
Concise Article
Submitted
05 Apr 2015
Accepted
12 May 2015
First published
27 May 2015

Med. Chem. Commun., 2015,6, 1190-1195

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