Burgos Miguel, Gil-Iturbe Eva, Idoate-Bayón Adrián, Castilla-Madrigal Rosa, Moreno-Aliaga Maria J, Lostao M Pilar
Center for Nutrition Research and Department of Nutrition, Food Science and Physiology; School of Pharmacy and Nutrition, University of Navarra, Pamplona, Spain.
IdiSNA, Navarra Institute for Health Research, Pamplona, Spain.
J Physiol Biochem. 2024 May 10. doi: 10.1007/s13105-024-01028-9.
Obesity constitutes a global health epidemic which worsens the main leading death causes such as type 2 diabetes, cardiovascular diseases, and cancer. Changes in the metabolism in patients with obesity frequently lead to insulin resistance, along with hyperglycemia, dyslipidemia and low-grade inflammation, favoring a more aggressive tumor microenvironment. One of the hallmarks of cancer is the reprogramming of the energy metabolism, in which tumor cells change oxidative phosphorylation to aerobic glycolysis or "Warburg effect". Aerobic glycolysis is faster than oxidative phosphorylation, but less efficient in terms of ATP production. To obtain sufficient ATP, tumor cells increase glucose uptake by the glucose transporters of the GLUT/SLC2 family. The human glucose transporter GLUT12 was isolated from the breast cancer cell line MCF7. It is expressed in adipose tissue, skeletal muscle and small intestine, where insulin promotes its translocation to the plasma membrane. Moreover, GLUT12 over-expression in mice increases the whole-body insulin sensitivity. Thus, GLUT12 has been proposed as a second insulin-responsive glucose transporter. In obesity, GLUT12 is downregulated and does not respond to insulin. In contrast, GLUT12 is overexpressed in human solid tumors such as breast, prostate, gastric, liver and colon. High glucose concentration, insulin, and hypoxia upregulate GLUT12 both in adipocytes and tumor cells. Inhibition of GLUT12 mediated Warburg effect suppresses proliferation, migration, and invasion of cancer cells and xenografted tumors. This review summarizes the up-to-date information about GLUT12 physiological role and its implication in obesity and cancer, opening new perspectives to consider this transporter as a therapeutic target.
肥胖是一种全球性的健康流行病,它加剧了2型糖尿病、心血管疾病和癌症等主要的致死原因。肥胖患者的代谢变化常常导致胰岛素抵抗,同时伴有高血糖、血脂异常和低度炎症,从而形成更具侵袭性的肿瘤微环境。癌症的一个标志是能量代谢重编程,其中肿瘤细胞将氧化磷酸化转变为有氧糖酵解或“瓦伯格效应”。有氧糖酵解比氧化磷酸化速度更快,但在产生三磷酸腺苷(ATP)方面效率较低。为了获得足够的ATP,肿瘤细胞通过GLUT/SLC2家族的葡萄糖转运蛋白增加葡萄糖摄取。人类葡萄糖转运蛋白GLUT12是从乳腺癌细胞系MCF7中分离出来的。它在脂肪组织、骨骼肌和小肠中表达,胰岛素可促进其向质膜转位。此外,在小鼠中过表达GLUT12可提高全身胰岛素敏感性。因此,GLUT12被认为是第二种胰岛素反应性葡萄糖转运蛋白。在肥胖状态下,GLUT12表达下调且对胰岛素无反应。相反,GLUT12在人类实体瘤如乳腺癌、前列腺癌、胃癌、肝癌和结肠癌中过表达。高糖浓度、胰岛素和缺氧均可上调脂肪细胞和肿瘤细胞中的GLUT12。抑制GLUT12介导的瓦伯格效应可抑制癌细胞和异种移植肿瘤的增殖、迁移和侵袭。本文综述了有关GLUT12生理作用及其在肥胖和癌症中的意义的最新信息,为将该转运蛋白作为治疗靶点提供了新的视角。