Fragment Evolution via Kinetic Target-Guided Synthesis for the Identification of Potent Bcl-2 Modulators

Tech ID: 13B140

­Competitive Advantages

  • Increased throughput by 200-fold
  • Can be applied to any biological target
  • Identifies previously "undruggable" targets
  • Increased sensitivity

Summary

USF researchers have developed an improved kinetic TGS sample detection method. This technology specifically targets modulating proteins of the Bcl-2 family. Bcl-2 is a protein coding gene that regulates cell death and is associated with many types of drug-resistant cancers and diseases. The identification of potent Bcl-2 inhibitors will assist in the development of new anticancer agents. This novel detection method utilizes liquid chromatography combined with MS/MS detection, making it more sensitive than current kinetic TGS methods. This technique improves the throughput by approximately 200-fold in comparison to conventional approaches, enabling 2000 fragment combinations to be screened in less than 12 hours. Further, this approach can be applied to any biological target including enzymes, protein-protein interactions, and protein-DNA/RNA interactions

A Schematic Representation of Kinetic TGS

Desired Partnerships

  • License
  • Sponsored Research
  • Co-Development