X Wang

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Jie Su

Jiangsu University of Science and Technology

Li Gf

Tan Cl

Zhang Xx

Zoucheng People's Hospital

Xie Ly

Changsong Wang

First Affiliated Hospital of Harbin Medical University

Zhang Dz

Yan Wen

Jiangsu University of Science and Technology

Xu Jl

Xi'an Chest Hospital

L Chang

Zigong First People's Hospital

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Jiangsu University of Science and Technology

Shanghai Jiao Tong University

Chinese Academy of Medical Sciences & Peking Union Medical College

Xi'an Chest Hospital

Shandong University of Traditional Chinese Medicine

Affiliated Hospital of Shandong University of Traditional Chinese Medicine

China Iron and Steel Research Institute Group

China Aerodynamics Research and Development Center

Northwestern Polytechnical University

First Affiliated Hospital of Hebei Medical University

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Fulvestrant inhibits the glycolysis of prolactinoma GH3 cells by downregulating IRE1/XBP1 signaling pathway.

PubMed (2018)

Changsong Wang Xu Jl Yan Wen Zhang Dz X Wang

We aimed to evaluate the effects of fulvestrant on the glycolysis of prolactinoma GH3 cells, and reveal the potential regulatory mechanisms.Prolactinoma cell line GH3 was treated with different concentrations of fulvestrant (0, 0.12, 0.25, 0.5 and 1 ng/ml) for 4 h. siRNAs XBP1s and XBP1u were constructed to treat GH3 cells. The expression levels of XBP1s, XBP1u, IRE1, PKM2 and GRP78 of GH3 cells were detected by Western blot. Meanwhile, the glycolytic activity of GH3 cells, including the glucose uptake, ATP/ADP, and lactate production were detected.The expression levels of XBP1s and XBP1u were significantly inhibited by fulvestrant in a dose-dependent manner. The glucose uptake, ATP/ADP and lactate production of GH3 cells were significantly inhibited by fulvestrant as well as siRNA XBP1s and XBP1u (p < 0.05). Western blot analysis suggested that the expression levels of IRE1, PKM2 and GRP78 were significantly decreased in GH3 cells treated by fulvestrant as well as siRNA XBP1s and XBP1u, compared with those in normal control (p < 0.05).Fulvestrant could inhibit the glycolysis of GH3 cells by downregulating IRE1/XBP1 signaling pathway, and this process was closely related with the downregulation of PKM2.

Fulvestrant

PKM2

XBP1

10.26355/eurrev_201808_15739

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