Invention:
This technology is a high-affinity E3-ligase binder, which has been optimized toward the specific proteolysis targeting chimera (PROTAC) mediated degradation of particular proteins. A PROTAC is a heterobifunctional molecule composed of two active domains and a linker, capable of removing specific unwanted proteins. This technology opens the door for the treatment of diseases and conditions otherwise thought to be untreatable or undruggable.
Background:
Once a target protein is identified as being associated with a disease, traditional drug discovery strategies have centered around finding an inhibitor to that protein. In many cases, such an approach involves screening a library of small-molecule drug candidates to identify those that bind to an active site on the target protein and modulate its activity. This traditional approach has certain limitations, which PROTACs can overcome. PROTAC degraders, together with related compounds like molecular glues and LYTACs, are the basic tools for a targeted protein degradation strategy. Research in this field is advancing rapidly, enabling the development of therapies for disease targets disease targets previously thought to be “undruggable.”
Applications:
- General drug discovery
- Cancer
- Chronic disease
Advantages:
- Overcomes the limitations of the traditional approach to disease treatment
- Can work well within complex signaling pathways
