Adaptive Targeted Protein Degradation System
Legal Citation
Summary of the Inventive Concept
A novel system for targeted protein degradation that utilizes adaptive E3 ubiquitin ligase proteins, conditional bifunctional constructs, and real-time monitoring to enhance precision, efficacy, and personalized treatment.
Background and Problem Solved
The original patent described compounds and methods for targeted degradation of enhancer of zeste homolog 2 polypeptide. However, these methods were limited by their static nature, lack of adaptability to cellular signals, and potential off-target effects. The new inventive concept addresses these limitations by introducing adaptive E3 ubiquitin ligase proteins that self-modify their substrate specificity in response to cellular signals, thereby enhancing precision and efficacy.
Detailed Description of the Inventive Concept
The new system comprises novel E3 ubiquitin ligase proteins engineered to exhibit conditional, cell-type specific activity. These proteins are designed to self-modify their substrate specificity in response to cellular signals, allowing for real-time adaptation to changing cellular conditions. The system also includes bifunctional constructs that bind target proteins and E3 ubiquitin ligase proteins, enabling targeted protein degradation. Additionally, a biosensor is integrated to detect the ubiquitination status of target proteins, enabling real-time monitoring and personalized adjustment of protein degradation therapies.
Novelty and Inventive Step
The new claims introduce adaptive E3 ubiquitin ligase proteins, conditional bifunctional constructs, and real-time monitoring, which are novel and non-obvious compared to the original patent. The inventive step lies in the integration of these components to create a dynamic, adaptive system for targeted protein degradation.
Alternative Embodiments and Variations
Alternative embodiments include the use of different E3 ubiquitin ligase proteins, conditional constructs, and biosensors. Variations may include the application of the system to different diseases or conditions, such as cancer, neurodegenerative disorders, or infectious diseases.
Potential Commercial Applications and Market
The adaptive targeted protein degradation system has significant commercial potential in the pharmaceutical and biotechnology industries, particularly in the development of personalized therapies for cancer and other diseases. The system's ability to adapt to changing cellular conditions and provide real-time monitoring capabilities makes it an attractive solution for precision medicine applications.
CPC Classifications
| Section | Class | Group |
|---|---|---|
| A | A61 | A61K31/166 |
| A | A61 | A61K31/351 |
| A | A61 | A61K31/405 |
| A | A61 | A61K38/45 |
| A | A61 | A61K47/545 |
| A | A61 | A61K47/55 |
| A | A61 | A61K47/555 |
| A | A61 | A61P35/00 |
| C | C07 | C07D401/14 |
| C | C07 | C07D405/12 |
| C | C07 | C07D405/14 |
| C | C07 | C07D409/14 |
| C | C07 | C07D417/14 |
| C | C07 | C07D471/04 |
| C | C12 | C12N9/1007 |
| C | C12 | C12Y201/01043 |
Original Patent Information
| Patent Number | US 11,857,519 |
|---|---|
| Title | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| Assignee(s) | Arvinas Operations, Inc. |