19.11.2021 - A deep-dive into SGLT1
SGLT1 - Sodium/Glucose Cotransporter 1 - SLC5A1
目标和家族:SGLT1属于溶质:钠转运体家族(SSSF,TCDB:2.A.21)。由于它是一种人体转运体,因此也被归类为SLC转运体:SGLT1相当于SLC5a1,属于钠/葡萄糖协同转运家族(SLC5)。
功能:通过Na+/K+ATP酶建立的钠跨膜梯度在小肠吸收D-葡萄糖。Na+/糖复合物以2:1的化学计量比出现。SGLT1是一种高亲和力/低容量转运蛋白,对其主要底物D-葡萄糖的亲和力为0.5 mM,转运速率为每秒20个分子。
生物体和定位:SGLT1是一种哺乳动物转运体,定位于小肠质膜内,特别是下段。在这里,高亲和力允许吸收D-葡萄糖,而SGLT2不吸收D-葡萄糖。SGLT1功能缺陷可导致先天性葡萄糖/半乳糖吸收不良(GGM),这是一种常染色体隐性疾病。
底物和抑制剂:d -葡萄糖是生理上最相关的底物。甲基- d -葡萄糖常用于SGLT1的实验,因为它不被代谢,但表现出与d -葡萄糖相似的转运特性。其他底物是半乳糖;d -木糖、2-脱氧- d -葡萄糖和3- o -甲基- d -葡萄糖也具有一定的转运活性。糖的运输与Na+转运耦合,但Na+可被Li+和H+所取代。表征良好的抑制剂是根根素,它在nM范围内对SGLT1的胞外位点有很高的亲和力,但对胞内位点的亲和力非常低。根皮素对SGLT1也有抑制作用,其IC50为~ 100 μ M。
相关转运蛋白:SGLT2与SGLT1的组织分布不同,主要在小肠上段表达。它具有较高的转运能力,但与d -葡萄糖的亲和力较低,Na+/ d -葡萄糖转运化学计量比为1:1。其他功能相关的转运蛋白属于GLUT家族,它们是人类d -葡萄糖单转运蛋白或SWEET家族,其中包含首次在植物中发现的糖转运蛋白。与此高度相关的还有来自大肠杆菌的典型且著名的细菌质子偶联乳糖转运蛋白LacY。
Read this publication - SSM-based electrophysiology, a label-free real-time method reveals sugar binding & transport events in SGLT1
Learn more from this Poster about a novel approach to detect electrogenic transporter activity in intact cells applied to investigate iPSC derived cardiomyocytes and neurons
SGLT1 - Current Traces after Application of alpha-MDG
SURFE2R N1 data and applications:
Current traces after application of 10 mM and 50 mM alpha-MDG.
2020 - A novel approach to detect electrogenic transporter activity in intact cells applied to investigate iPSC derived cardiomyocytes and neurons
SURFE²R N1 and SURFE²R 96SE poster, 64th Annual Meeting of the Biophysical Society (1.6 MB)
2017 - An emerging technique for the characterization of transport proteins: SSM-based electrophysiology
SURFE²R N1 and SURFE²R SE96 poster, 19th IUPAB / 11th EBSA congress 2017 (3.3 MB)
2015 - Studying Electrogenic Transporters of the SLC Family in a Parallel Way Utilizing Solid Supported Membrane Technology
SURFE²R N96 poster (a predecessor model of the SURFE²R 96SE) Biophysics 2015 (0.8 MB)