Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer.
Cyanidin-3-o-glucoside directly binds to ERα36 and inhibits EGFR-positive triple-negative breast cancer.
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Cyanidin-3-o-glucoside 直接结合 ER α 36 并抑制 EGFR 阳性三阴性乳腺癌
DOI：
10.18632/oncotarget.12025
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发表时间：
2016-10-18
期刊：
影响因子：
--
通讯作者：
Li X
中科院分区：
文献类型：
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作者：
Wang L;Li H;Yang S;Ma W;Liu M;Guo S;Zhan J;Zhang H;Tsang SY;Zhang Z;Wang Z;Li X;Guo YD;Li X
花青素已被证明可以抑制乳腺癌（BC）细胞的生长和转移潜力。然而，尚未研究单个花青素对三阴性乳腺癌（TNBC）的影响。在本研究中，我们发现矢车菊素-3-o-葡萄糖苷（Cy-3-glu）优先促进共表达雌激素受体α 36（ERα36）和表皮生长因子受体（EGFR）的TNBC细胞的凋亡。我们证明，Cy-3-glu直接结合ERα36的配体结合结构域（LBD），抑制EGFR/AKT信号传导，并促进EGFR降解。我们还证实了Cy-3-glu在异种移植小鼠模型中对TNBC的治疗功效。我们的数据表明，Cy-3-glu可能是一种新的针对TNBC共表达的ERα36/EGFR的预防/治疗剂。
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.