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钠-葡萄糖协同转运蛋白2及其抑制剂与相关疾病

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葡萄糖(glucose)是生物最主要的供能物质,是活细胞的能量来源和新陈代谢的中间产物,并在细胞信号传递中发挥着重要作用。异常葡萄糖代谢经常与糖尿病、视网膜病变、阿尔兹海默症以及心血管疾病等相关。钠-葡萄糖协同转运蛋白2(sodium-glucose cotransporter 2,SGLT2)是机体内参与维持葡萄糖稳态的转运体之一,介导肾对葡萄糖的重吸收,对维持血浆葡萄糖稳定有着重要作用。钠-葡萄糖协同转运蛋白2抑制剂(sodium-glucose cotransporter 2 inhibitor,SGLT2i)可减少肾对葡萄糖的重吸收,对于血糖、血压、体重等产生积极影响。本文总结了当前SGLT2及其抑制剂的研究进展,综述了 SGLT2结构及关键位点、SGLT2i作用机制,特别是近几年的研究发现,SGLT2i对肾及心血管的保护作用愈加明显,同时还能抵抗肿瘤细胞的发生和发展。最后,本文总结讨论了目前针对SGLT2i相关研究的瓶颈问题,为未来基于结构的抑制剂药物优化提供新思路。
Sodium-Glucose Cotransporter 2 and Its Inhibitors with Related Diseases
Glucose is the most important biological energy donor,is the source of energy and metabolism of living cells,and plays an important role in cell signaling.Abnormal glucose metabolism is frequently associated with diabetes mellitus,retinopathy,Alzheimer's disease,and cardiovascular diseases.Sodi-um-glucose cotransporter 2(SGLT2)is one of the transporters involved in the maintenance of glucose ho-meostasis.It mediates the reabsorption of glucose by the kidney and plays an important role in maintai-ning the stability of plasma glucose.Sodium-glucose cotransporter 2 inhibitors(SGLT2i)can reduce the reabsorption of glucose in the kidney and have a positive impact on blood glucose,blood pressure,body weight,etc.This paper summarizes the current research progress of SGLT2 and its inhibitors,the struc-ture and key sites of SGLT2 and the mechanism of SGLT2i.In particular,in recent years,it is found that the protective effect of SGLT2i on kidney and cardiovascular is more obvious,and it can also resist the occurrence and development of tumor cells.Finally,this paper summarises and discusses the current bot-tlenecks in research related to SGLT2i and provides new ideas for future structure-based drug optimisation of inhibitors.

glucose metabolismsodium-glucose cotransporter 2(SGLT2)sodium-glucose cotransport-er 2 inhibitor(SGLT2i)cardiovascular and kidneycancer

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天津大学生命科学学院结构生物学实验室,天津 300072

葡萄糖代谢 钠-葡萄糖协同转运蛋白2 钠-葡萄糖协同转运蛋白2抑制剂 心血管和肾 癌症

2024

中国生物化学与分子生物学报
中国生物化学与分子生物学会 北京大学

中国生物化学与分子生物学报

CSTPCD北大核心
影响因子:0.617
ISSN:1007-7626
年,卷(期):2024.40(2)
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