Center for Molecular Medicine, China Medical University Hospital Taichung 404, Taiwan ; Graduate Institute of Cancer Biology, China Medical University Taichung 404, Taiwan ; the Ph.D. program for Cancer Biology and Drug Discovery, China Medical University Taichung 404, Taiwan ; Department of Biotechnology, Asia University Taichung 413, Taiwan.
Am J Transl Res. 2013 May 24;5(4):441-9. Print 2013.
Sodium/glucose co-transporter 1 (SGLT1), which actively and energy-dependently uptakes glucose, plays critical roles in the development of various diseases including diabetes mellitus and cancer, and has been viewed as a promising therapeutic target for these diseases. Protein-protein interaction with EGFR has been shown to regulate the expression and activity of SGLT1. Exogenous expression of SGLT1 is one of the essential approaches to characterize its functions; however, exogenously expressed SGLT1 is not firmly detectable by Western blot at its calculated molecular weight, which creates a hurdle for further understanding the molecular events by which SGLT1 is regulated. In this study, we demonstrated that exogenous SGLT1 functions in glucose-uptake normally but is consistently detected near the interface between stacking gel and running gel rather than at the calculated molecular weight in Western blot analysis, suggesting that the overexpressed SGLT1 forms SDS-resistant aggregates, which cannot be denatured and effectively separated on SDS-PAGE. Co-expression of EGFR enhances both the glucose-uptake activity and protein level of the SGLT1. However, fusion with Flag or HA tag at its carboxy- but not its amino-terminus abolished the glucose-uptake activity of exogenous SGLT1 without affecting its protein level. Furthermore, the solubility of SGLT1 aggregates was not affected by other detergents but was partially improved by inhibition of o-link glycosylation. These findings suggested exogenous overexpression of SGLT1 can function normally but may not be consistently detectable at its formula weight due to its gel-shift behavior by forming the SDS-resistant aggregates.
钠-葡萄糖共转运蛋白 1(SGLT1)可主动且依赖能量摄取葡萄糖,在包括糖尿病和癌症在内的多种疾病的发生发展中发挥着关键作用,已被视为这些疾病有希望的治疗靶点。有研究表明,SGLT1 与表皮生长因子受体(EGFR)的蛋白-蛋白相互作用可调节 SGLT1 的表达和活性。外源性表达 SGLT1 是其功能特征分析的基本方法之一;然而,在 Western blot 分析中外源表达的 SGLT1 并不能在其计算的分子量处被牢固检测到,这给进一步了解 SGLT1 调节的分子事件带来了障碍。在本研究中,我们证明了外源性 SGLT1 能够正常发挥葡萄糖摄取功能,但在 Western blot 分析中始终在堆积胶和运行胶之间的界面处而非在计算的分子量处被检测到,这表明过表达的 SGLT1 形成了 SDS 抗性聚集体,不能在 SDS-PAGE 上变性并有效分离。EGFR 的共表达可增强 SGLT1 的葡萄糖摄取活性和蛋白水平。然而,与 Flag 或 HA 标签融合在其羧基端而非氨基端则会消除外源性 SGLT1 的葡萄糖摄取活性而不影响其蛋白水平。此外,SGLT1 聚集体的溶解度不受其他去污剂的影响,但通过抑制 O-连接糖基化可部分改善。这些发现表明,外源性过表达的 SGLT1 可以正常发挥作用,但由于其形成 SDS 抗性聚集体的胶移行为,可能无法始终在其分子量处被检测到。