Macrophage-Targeted mTor Chemical Conjugates for Therapy and Imaging
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Solution Overview
Problem
There is a need for compounds that can specifically target macrophages for the treatment of inflammatory diseases, immune diseases, and other macrophage-related disorders, as well as for inhibitors and modulators of the mammalian target of rapamycin (mTor) that can enter macrophages and function as imaging agents.
Innovation Solution
The development of a compound of Formula 1, which includes specific structural elements such as X, Y, Z, L, R1-R5, n, and Q, capable of entering macrophages and modulating mTor activity, while also serving as an imaging agent.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If conventional mTor inhibitors are used, then mTor activity can be modulated, but they cannot specifically target macrophages or serve as imaging agents
Solution Approach 1:
The patent combines three distinct functions into a single molecular conjugate: (1) mTor inhibition capability through the rapamycin derivative, (2) macrophage targeting through the transferrin receptor-binding moiety, and (3) imaging capability through the attached imaging agent. This merging resolves the contradiction by creating a multi-functional molecule that simultaneously achieves modulation, targeting, and imaging without requiring separate administration of multiple agents.
Solution Approach 2:
The chemical conjugate of Formula (1) is designed as a universal platform where different imaging agents can be attached to the same mTor inhibitor-macrophage targeting core structure. This universal design allows the same conjugate framework to serve multiple purposes (therapy and diagnostics) and enables flexibility in selecting imaging modalities without redesigning the entire molecular architecture.
2Measurement precision
If compounds are designed to specifically target macrophages, then macrophage-related diseases can be treated, but the compounds cannot simultaneously function as imaging agents
Solution Approach 1:
The patent uses a linker moiety as an intermediary component that connects the mTor inhibitor-macrophage targeting complex to the imaging agent. This intermediary structure allows the imaging agent to be attached without interfering with the macrophage targeting or mTor inhibition functions, thereby enabling imaging capability while maintaining the integrity of the therapeutic components.
Solution Approach 2:
The chemical conjugate represents a composite molecular structure combining organic chemistry components (mTor inhibitor, targeting moiety, linker) with imaging agent components. This composite approach allows integration of materials with different functions (therapeutic and diagnostic) into a single hybrid molecule that exhibits both therapeutic and imaging properties.
3Ease of operation
If mTor inhibitors are administered systemically, then they can reach macrophages, but they lack specific targeting and imaging capability
Solution Approach 1:
The patent imparts local quality to the mTor inhibitor by attaching a macrophage-specific targeting moiety (transferrin receptor binder) to the general mTor inhibitor structure. This creates a molecule with differentiated regions: one part that binds mTor universally and another part that specifically recognizes macrophage transferrin receptors, thereby achieving specific targeting while maintaining ease of systemic administration.
Data Source
AI summary
The present invention relates to compounds, and methods of use thereof, capable of entering macrophages. The invention further relates to compounds capable of modulating (for example inhibiting) the activity of the mammalian target of rapamycin (mTor), treating mTor-associated diseases, in particular, but not limited to, related to mTor in macrophages. The invention also relates to compounds capable of imaging mTor in a subject, in particular, but not limited to, mTor in macrophages.