OmniTAC Protein Recruiters for Targeted Intracellular Modification
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Solution Overview
Problem
Current drug approaches for modifying proteins are limited by small molecules' narrow method of action, poor oral bioavailability of biologics, and difficulty in targeting intracellular targets, necessitating a more specific and potent therapeutic solution.
Innovation Solution
Development of OmniTAC compounds comprising a targeting ligand, a linker, and a recruiting ligand that bring a target protein into proximity with a modifier protein to induce specific modifications, leveraging the protein's modification capabilities.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If small molecules are used to modify proteins, then the method of action is narrow, but the oral bioavailability is poor
Solution Approach 1:
The invention divides the therapeutic agent into two separate components: a small molecule protein modifier with narrow but potent mechanism of action, and a protein carrier with good oral bioavailability. The small molecule segment performs the specific modification function while the protein carrier segment enables oral delivery, resolving the contradiction between versatility and reliability.
Solution Approach 2:
The protein carrier acts as an intermediary that delivers the small molecule protein modifier to the target site after oral administration. This mediator enables the small molecule to overcome its poor oral bioavailability while maintaining its narrow but effective method of action for protein modification.
2Reliability
If biologics are used to modify proteins, then the oral bioavailability is improved, but the method of action becomes less specific
Solution Approach 1:
The invention segments the biologic into a protein carrier component that provides oral bioavailability and a small molecule protein modifier component that provides specific method of action. This segmentation allows each component to excel at its designated function without compromising the other.
Solution Approach 2:
The invention applies local quality by assigning different functional properties to different parts of the conjugate: the protein carrier portion provides oral bioavailability while the small molecule modifier portion provides specific protein modification capability, allowing each part to optimize its local function.
3Ease of operation
If conventional therapies are used, then the treatment is easier to administer, but the ability to target intracellular targets is limited
Solution Approach 1:
The protein carrier serves as an intermediary that facilitates cellular uptake of the small molecule protein modifier. This mediator enables the conjugate to target intracellular proteins while maintaining ease of oral administration, overcoming the limitation of conventional therapies.
Data Source
AI summary
Provided are compounds that may bind a target protein, and result in modification of the target protein. The compounds may further bind a modifier protein. The modifier protein may carry out or enhance the modification of the target protein. The modification may activate or reactivate the target protein. Also provided are methods of using the compounds.