Chemically Modified Aptamers for Specific Microvesicle Targeting
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Solution Overview
Problem
Current diagnostic and therapeutic methods for diseases such as cancer lack specificity and efficacy, particularly in targeting microvesicle surface antigens, and existing aptamers face challenges in scalability, toxicity, and immunogenicity.
Innovation Solution
Development of chemically modified oligonucleotide aptamers that specifically bind to microvesicle surface antigens, including nucleolin, for diagnostic and therapeutic applications, with the ability to inhibit nucleolin activity and induce apoptosis in cancer cells, and the use of multipartite constructs for targeted delivery of chemotherapeutic agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If chemically modified oligonucleotide aptamers are used to bind microvesicle surface antigens, then specificity and affinity are improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies chemical modifications to the oligonucleotide aptamers, changing their chemical parameters to improve binding specificity and affinity for microvesicle surface antigens. This involves altering the molecular structure through chemical means while maintaining the core binding function.
Solution Approach 2:
The patent creates composite structures by combining oligonucleotide aptamers with chemical modifications, resulting in hybrid molecules that integrate the specificity of nucleic acid binding with the enhanced stability and affinity provided by chemical modifications.
2Reliability
If aptamers are used for targeted delivery of chemotherapeutic agents, then therapeutic efficacy is improved, but toxicity increases
Solution Approach 1:
The patent uses oligonucleotide aptamers as intermediary molecules that specifically bind to microvesicle surface antigens, enabling targeted delivery of chemotherapeutic agents to cancer cells while minimizing exposure to healthy tissues. This mediator approach reduces off-target toxicity.
Solution Approach 2:
The patent achieves localized therapeutic action by directing chemotherapeutic agents specifically to cancer cells through aptamer-mediated targeting. The therapeutic effect is concentrated at the target site (local quality) rather than being distributed systemically, thereby reducing overall toxicity.
3Object-generated harmful factors
If aptamers are used instead of monoclonal antibodies, then immunogenicity is reduced, but binding affinity may be compromised
Solution Approach 1:
The patent enhances the binding parameters of oligonucleotide aptamers through chemical modifications, improving their affinity and specificity to match or exceed that of monoclonal antibodies while maintaining the low immunogenicity inherent to nucleic acid-based therapeutics.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The aptamers provide high specificity and affinity for microvesicle surface antigens, enabling effective diagnostics and therapeutics, with improved scalability, reduced toxicity, and enhanced penetration into constricted areas, while allowing for targeted delivery of chemotherapeutics.
Implementation Method 1
Aptamers are oligomeric nucleic acid molecules having specific binding affinity to molecules, which may be through interactions other than classic Watson-Crick base pairing
Implementation Method 2
the ability to inhibit nucleolin activity and induce apoptosis in cancer cells
Data Source
AI summary
Methods and compositions are provided for oligonucleotides that bind targets of interest. The targets include cells and microvesicles, such as those derived from various diseases. The oligonucleotides can be used for diagnostic and therapeutic purposes. The target of the oligonucleotides can be a target such as PARP1, HIST1H1B, HIST1H1D, NCL, FBL, SFPQ, RPL12, ACTB, HIST1H4A, SSBP1, NONO, H2AFJ, and DDX21, or a complex, subunit or fragment thereof.