Liu Liyan, Zhou Yutao, Liu Jing, Zhang Xinmiao, He Chongwu, Zeng Xiaoqiang, Dejenie Rebeka, Zeb Usman, Zeng Qiao, Liu Lan, Li Jianglong, Zeng Xingsheng, Hu Qinglong, Huang Xianming, Xu Xue, Dong Hanzhi, Zhong Jinxiu, Huang Yanxiao, Lv Qiaoli, Liu Bo, Qiu Yu-An, Yu Tenghua
Department of Pharmacy, Jiangxi Cancer Hospital & Institute, The Second Affiliated Hospital of Nanchang Medical College, Jiangxi Key Laboratory of Oncology (2024SSY06041), Jiangxi Clinical Research Center for Cancer, JXHC Key Laboratory of Tumor Microenvironment and Immunoregulation, Jiangxi Key Laboratory of Tumor Metastasis of Jiangxi Health Commission, Nanchang, 330029, China.
School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang, 330004, China.
J Transl Med. 2025 Aug 26;23(1):960. doi: 10.1186/s12967-025-07005-0.
G protein-coupled estrogen receptor (GPER) significantly influences metabolic regulation by engaging multiple signaling pathways that affect overall metabolic health. Its structure and signaling mechanisms drive its diverse roles. Our team and others have successfully demonstrated that GPER modulates nutrient metabolism, spanning glucose, protein, and lipid metabolism, while also contributing to vitamin and mineral metabolism. Studies have linked GPER to metabolic disorders, including type 2 diabetes, nonalcoholic fatty liver disease, metabolic syndrome, and cardiovascular diseases, as well as thyroid disorders, highlighting its wide-reaching metabolic impact. GPER holds promise for energy balance and weight management by regulating energy expenditure and thermogenesis. Moreover, it appears to influence the metabolism of cancer cells during tumor progression. Rapid advancements in GPER agonist and antagonist research have highlighted the therapeutic potential of GPER agonists for treating metabolic diseases. Further investigations into GPER biology, mechanisms, and clinical applications will support novel therapeutic strategies, establishing GPER as a key target in metabolic research and treatment.
G蛋白偶联雌激素受体（GPER）通过参与多种影响整体代谢健康的信号通路，对代谢调节产生显著影响。其结构和信号传导机制决定了它的多种作用。我们团队以及其他研究团队已成功证明，GPER可调节营养物质代谢，涵盖葡萄糖、蛋白质和脂质代谢，同时也对维生素和矿物质代谢有作用。研究已将GPER与多种代谢紊乱联系起来，包括2型糖尿病、非酒精性脂肪性肝病、代谢综合征和心血管疾病，以及甲状腺疾病，凸显了其广泛的代谢影响。GPER有望通过调节能量消耗和产热来实现能量平衡和体重管理。此外，它似乎在肿瘤进展过程中影响癌细胞的代谢。GPER激动剂和拮抗剂研究的迅速进展突出了GPER激动剂在治疗代谢性疾病方面的治疗潜力。对GPER生物学、机制和临床应用的进一步研究将支持新的治疗策略，确立GPER作为代谢研究和治疗的关键靶点。
