Novel Technology to Monitor Membrane Protein Trafficking for Drug Discovery and Drug Development
High-throughput screening (HTS) has enabled successful unbiased drug-discovery and development of novel therapies. Much of its success has to do with the membrane proteins targeted, and the drugs directed to receptors that have underlying roles in a myriad of diseases,including cancer, heart disease, diabetes, and mental illness. Therefore, membrane proteins represent a goldmine of targets that must be screened to fully exploit their rich therapeutic potential. However, current HTS technology has limitations. HTS becomes particularly challenging for those receptors that are of great therapeutic interest but have non-canonical signaling or remain uncharacterized. This technology takes advantage of the universal feature of membrane receptor protein regulation and providesadditional solutions to plasma membrane trafficking. Current HTS trafficking screens are restricted by a lack of reagent universality, high costs of imaging equipment, and the need of sophisticated deconvolution algorithms to identify subpopulations of membrane proteins. This technology relies upon a new class of assay able to monitor in real-time membrane protein trafficking by the simple addition of the corresponding drug without the need for reagent washes or highly automated equipment.
Applications
  • Screening binding agents for binding to cell membrane proteins
  • Identifying novel drugs for diseases such as cancer, diabetes, autoimmune diseases, heart diseases, mental illness, and microbial infections
  • Evaluating drug candidates for the treatment or prevention of various diseases including coronavirus and COVID-19
Problems Addressed
  • Mimics physiological conditions better, having greater specificity to target molecules than traditional human-made sensors
  • Process is in real-time in live cells while current technologies only measure end point
Competitive Advantages
  • Current plasma membrane protein drug discovery assays are highly idiosyncratic and require specialized protocol development
  • Current HTS technologies are restricted due to lack of reagent universality, high costs of imaging equipment, and confounding high background fluorescence
Patents
  • 63/115,827 (Provisional, Pending)

Case ID
2021-008
Inventor
Bradley K. McConnell
Professor, Pharmacological and Pharmaceutical Studies
Category