A cell-based fluorescent glucose transporter assay for SGLT2 inhibitor discovery

Abstract

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-1,3-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.

Keywords

• SGLT2 inhibitor
• NBDG
• Type 2 diabetes mellitus
• Kidney