Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer

花青素-3-o-葡萄糖苷直接与 ERα36 结合并抑制 EGFR 阳性三阴性乳腺癌

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作者:Li Wang, Haifeng Li, Shiping Yang, Wenqiang Ma, Mei Liu, Shichao Guo, Jun Zhan, Hongquan Zhang, Suk Ying Tsang, Ziding Zhang, Zhaoyi Wang, Xiru Li, Yang-Dong Guo, Xiangdong Li

Abstract

Anthocyanins have been shown to inhibit the growth and metastatic potential of breast cancer (BC) cells. However, the effects of individual anthocyanins on triple-negative breast cancer (TNBC) have not yet been studied. In this study, we found that cyanidin-3-o-glucoside (Cy-3-glu) preferentially promotes the apoptosis of TNBC cells, which co-express the estrogen receptor alpha 36 (ERα36) and the epidermal growth factor receptor (EGFR). We demonstrated that Cy-3-glu directly binds to the ligand-binding domain (LBD) of ERα36, inhibits EGFR/AKT signaling, and promotes EGFR degradation. We also confirmed the therapeutic efficacy of Cy-3-glu on TNBC in the xenograft mouse model. Our data indicates that Cy-3-glu could be a novel preventive/therapeutic agent against the TNBC co-expressed ERα36/EGFR.

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