6241 – A Real-Time FRET Assay for Use in High Throughput Screening of Potential GLS1 Inhibitors

Simple fluorescence assay techniquesReal-time kinetics measurement of GLS catalysis
  • Simple fluorescence assay techniques
  • Real-time kinetics measurement of GLS catalysis

Abstract:

Invention Summary

An approach to label glutaminase (GLS1) protein with a fluorescent reporter group that allows for real-time monitoring of glutaminase activation and inhibition by small molecules.

Technology Overview

Glutamine metabolism is essential to promote cancer cell growth, proliferation, and migration
The mitochondrial enzyme glutaminase (GLS) has been identified as a therapeutic target for cancer and small molecule inhibitors that target this enzyme offer new opportunities in the development of cancer drugs
Little is known regarding how small molecules bind to GLS isoforms and the mechanisms by which they block activation
Cornell researchers have developed a method to label monomers and dimers of GLS with a fluorescent reporter group to screen for compounds that bind to the GLS protein
Fluorescence signal from labeled GLS protein can be monitored in real time to evaluate enzyme activity in response to small molecule inhibitors.

Website:

https://cornell.flintbox.com/technologies/E3940E108B3C42F987CC4E2463AD0F2A

Advantages:

  • Simple fluorescence assay techniques
  • Fluorescent reporter does not interfere with GLS activity

Potential Applications:

  • A screening kit for compounds that inhibit or stabilize GLS tetramer formation
  • Real-time kinetics measurement of GLS catalysis

Contact Information:

Name: Phillip Owh

Title :

Department :

Email : po62@cornell.edu

Phone : 1-607-254-4508

Address :