Liposome-based high-throughput screening platform for identifying SGLT1 and GLUT5 competitors and activators

Overview

This solution offers a liposome-based high-throughput screening platform designed to identify competitors and activators of two important human sugar transporters: SGLT1 (sodium-glucose linked transporter 1) and GLUT5 (glucose transporter 5). By embedding these transmembrane proteins within synthetic phospholipid-cholesterol liposomes, the platform preserves their native structure and function, enabling reliable screening of nutritionally relevant compounds. The technology is particularly valuable for food, nutrition, and pharmaceutical companies seeking to understand how natural and synthetic ingredients interact with sugar uptake pathways, with applications in sweetener discovery, metabolic health research, and dietary intervention strategies.

Technical specifications

Core technology:

• Fluorescent dye-entrapping liposomes (~1 million dye molecules per liposome) incorporating recombinant or cell-membrane-derived SGLT1 and GLUT5
• Phospholipid-cholesterol bilayer that maintains transmembrane proteins in a near-native lipid environment
• Biotin-PEG immobilized analogs of glucose and fructose on streptavidin-coated microplates
• Competitive binding assay format: competitors reduce and enhancers increase receptor-mediated liposome binding, producing an inverse fluorescence signal upon liposome lysis

Key features:

• High-throughput microplate format with quantitative fluorescence readout
• Liposome stability exceeding one year at 21°C and functional binding retention for at least 10 years at 4°C
• Specificity, inhibition, and activation protocols already established from prior bacterial receptor work
• Amenable to automation and screening of natural sample matrices including GRAS (Generally Recognized as Safe) ingredients
• Equilibrium filtration validation for confirming successful protein incorporation

Prior validation:

• Successfully applied to bacterial periplasmic binding proteins for maltose and thiamine detection, demonstrating exquisite specificity versus structurally similar sugars and analogs
• 23 years of liposome-based assay development experience

Technology readiness level

The liposome platform itself is fully developed and validated for bacterial receptors against non-immunogenic small molecule nutrients. The extension to human sugar transporters SGLT1 and GLUT5 is at an early stage. Next steps include securing a recombinant source of SGLT1 and GLUT5 (or alternatively incorporating cell membrane components from expressing cultures), modifying established protocols for transmembrane protein incorporation, generating immobilized glucose and fructose analogs, and vetting the competitive assay using sugar analogs and nutritionally relevant competitors and enhancers. The platform is ready for sponsored research collaboration to advance validation toward broader screening applications.