The sodium/glucose cotransporter 2(SGLT2)is responsible for the majority of glucose reabsorption in the kidney,and currently,SGLT2 inhibitors are considered as promising hypoglycemic agents for the treatment of type 2...The sodium/glucose cotransporter 2(SGLT2)is responsible for the majority of glucose reabsorption in the kidney,and currently,SGLT2 inhibitors are considered as promising hypoglycemic agents for the treatment of type 2 diabetes mellitus.By constructing CHO cell lines that stably express the human SGLT2 transmembrane protein,along with a fluorescent glucose transporter assay that uses 2-[N-(7-nitrobenz-2-oxa-l,3-diazol-4-yl)amino]2-deoxyglucose(2-NBDG)as a glucose analog,we have developed a nonradioactive,cell-based assay for the discovery and characterization of SGLT2 inhibitors.展开更多
基金supported by Beijing Natural Science Foundation(No.7102118)the Key Project of the National Twelfth-Five Year Research Program of China and National S&T Major Special Project on Major New Drug Innovation(No.2012ZX09301002-004).
文摘The sodium/glucose cotransporter 2(SGLT2)is responsible for the majority of glucose reabsorption in the kidney,and currently,SGLT2 inhibitors are considered as promising hypoglycemic agents for the treatment of type 2 diabetes mellitus.By constructing CHO cell lines that stably express the human SGLT2 transmembrane protein,along with a fluorescent glucose transporter assay that uses 2-[N-(7-nitrobenz-2-oxa-l,3-diazol-4-yl)amino]2-deoxyglucose(2-NBDG)as a glucose analog,we have developed a nonradioactive,cell-based assay for the discovery and characterization of SGLT2 inhibitors.