Dongliang Zhu^1,*, Jun Yang², Jiaxin Xu³

Oncologie, Vol.24, No.3, pp. 471-482, 2022, DOI:10.32604/oncologie.2022.024062

Abstract G-protein coupled estrogen receptor (GPER) is a transmembrane receptor that mediates non-genomic effects of estrogen. This study aimed to investigate the role of GPER in the stemness formation and malignancies in triple negative breast cancer (TNBC) cells. Spheroids of MDA-MB-468 cells were induced by mammosphere culture, and the proportion of the CD44⁺ /CD24^−/low stem cell subpopulation was detected. Malignant characteristics, expression of GPER and stemness-related markers, and tumorigenesis in a xenograft assay were compared between the mammospheres and adherent cultured cells. The impacts of 17β-estradiol (E2) and the GPER-specific antagonist G15 were studied in in vitro assays. The proportion of… More >

Changyu Liu^*, Yongde Liao^*, Sheng Fan^*, Xiangning Fu^*, Jing Xiong^†, Sheng Zhou^†, Man Zou^‡, Jianmiao Wang^§

Oncology Research, Vol.27, No.3, pp. 283-292, 2019, DOI:10.3727/096504017X15035795904677

Abstract G-protein-coupled estrogen receptor (GPER) was found to promote non-small cell lung cancer (NSCLC) by estrogen, indicating the potential necessity of inhibiting GPER by a selective antagonist. This study was performed to elucidate the function of GPER-selective inhibitor G15 in NSCLC development. Cytoplasmic GPER (cGPER) and nuclear GPER (nGPER) were detected by immunohistochemical analysis in NSCLC samples. The relation of GPER and estrogen receptor (ER ) expression and correlation between GPER, ER , and clinical factors were analyzed. The effects of activating GPER and function of G15 were analyzed in the proliferation of A549 and H1793 cell lines and development of… More >