Cyclic Dinucleotide Conjugates for Tumor-Targeted Imaging
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Solution Overview
Problem
Current tumor-targeted imaging agents have low selectivity for cancer tissues, leading to low signal-to-noise ratios and side effects due to widespread distribution in the body, making it difficult to accurately diagnose and treat cancer.
Innovation Solution
Development of cyclic dinucleotide conjugates that selectively accumulate in tumor tissues with high efficiency, conjugated with imaging and therapeutic moieties such as Cy7 and Dy547, allowing for targeted imaging and therapeutic delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If current imaging agents are used, then they can be distributed throughout the body for imaging, but they accumulate in normal healthy tissues resulting in low signal to noise ratio and side effects
Solution Approach 1:
The patent applies local quality by designing imaging agents with specific molecular structures (cyclic dinucleotide conjugates) that have different distribution characteristics compared to conventional agents. The conjugates are engineered to preferentially accumulate in tumor tissues through interactions with cancer-specific molecules, creating high signal-to-noise ratios in tumor regions while minimizing accumulation in normal tissues, thus reducing side effects.
Solution Approach 2:
The patent uses cyclic dinucleotide conjugates as intermediary substances that mediate between the imaging agent and tumor tissues. These conjugates act as carriers that selectively deliver imaging moieties to tumor cells through specific binding interactions, enabling targeted imaging while avoiding non-specific accumulation in healthy tissues.
2Measurement precision
If highly selective ligands are developed to achieve high tumor/normal tissue contrast, then imaging precision improves, but the complexity of developing and validating such ligands increases
Solution Approach 1:
The patent applies parameter changes by systematically varying molecular parameters of the cyclic dinucleotide conjugates, such as the type of nucleotide bases, sugar moieties, and conjugation linkers. By optimizing these parameters, the patent achieves high tumor/normal tissue contrast while maintaining a manageable development process, as the conjugate structure follows established medicinal chemistry principles rather than requiring entirely new ligand classes.
Data Source
AI summary
This invention is in the field of medicinal chemistry and relates to a new class of cyclic dinucleotide conjugates (e.g., Formula I) which function as tumor-targeted imaging agents, and their use in diagnostic and therapeutic intervention for disorders (e.g., cancer).