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A Method of Creating FKBP-Small Molecule Composite Surfaces as Inhibitors of Protein-Protein Interactions

Life Sciences
Small Molecules
Therapeutics
Drugs / Pharmaceuticals
College
College of Medicine (COM)
Researchers
Briesewitz, Roger
Pei, Dehua
Wu, Xianghong
Licensing Manager
Flammang, Ann Marie
614-292-9839
flammang.2@osu.edu

TS-037677 — A mechanism by which the inhibiting effects of drugs and other molecules on protein-protein interactions can be measured.

Protein-protein interactions (PPIs) occur when two or more proteins bind together, and they represent a large group of drug targets. However, PPIs are difficult to disrupt because they usually involve large, two-dimensional target surfaces. Conventional small molecule drugs can bind with high affi…

The Need

Protein-protein interactions (PPIs) occur when two or more proteins bind together, and they represent a large group of drug targets. However, PPIs are difficult to disrupt because they usually involve large, two-dimensional target surfaces. Conventional small molecule drugs can bind with high affinity in deep protein pockets which provide a three-dimensional binding space. In contrast, the flat, two-dimensional target surfaces of PPIs do not allow the establishment of sufficient drug-target interactions to support high affinity binding of small molecules. Thus, most PPIs are “undruggable” with traditional small molecules so the development of small molecules that can inhibit PPIs could be of great benefit. This invention proposes the small molecule technology to discover drugs targeting protein-protein interactions.

The Technology

Ohio State University researchers, led by Dr. Roger Briesewitz, have discovered a generalized mechanism by which the inhibiting effects of drugs and other molecules on protein-protein interactions can be measured. The researchers have generalized the mechanism of action of FK506 and rapamycin to create libraries of novel small molecules that have the potential to contain inhibitors of otherwise undruggable protein-protein interactions.

Commercial Applications

  • Anti-cancer drugs
  • Therapeutics for disease treatment

Benefits/Advantages

  • Small molecule based technology that can be used to discover inhibitors of protein-protein interactions