Multivalent Synthetic Ligands Targeting Surface Nucleolin
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Solution Overview
Problem
Current anti-cancer molecules lack specificity, leading to significant side effects and are inefficient in inhibiting both tumour cell proliferation and angiogenesis, with existing treatments requiring conventional chemotherapy or radiotherapy and facing challenges in bioavailability and industrial scalability.
Innovation Solution
Development of multivalent synthetic compounds with pseudopeptide units grafted onto a support, specifically targeting surface nucleolin, which are resistant to proteases and have improved bioavailability, allowing for dual inhibition of tumour proliferation and angiogenesis without the need for conventional treatments.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional anti-cancer molecules are used, then tumour cell proliferation is inhibited, but side effects increase due to lack of specificity
Solution Approach 1:
The invention segments the anti-cancer function into two distinct molecular activities: anti-mitotic activity (inhibiting cell division) and anti-angiogenic activity (inhibiting blood vessel formation). By combining these two functions in a single molecule, the patent achieves both tumour cell proliferation inhibition and angiogenesis blocking, thereby improving anti-cancer efficacy while reducing side effects through targeted dual-action therapy
Solution Approach 2:
The patent creates a universal anti-cancer molecule that performs multiple functions simultaneously: it acts as both an anti-mitotic agent and an anti-angiogenic agent. This multi-functional molecule targets both tumour cells and the angiogenesis process, providing comprehensive cancer treatment in a single therapeutic agent, thus improving reliability while maintaining selectivity
2Reliability
If monospecific anti-angiogenic molecules are used, then one angiogenic factor is inhibited, but resistance develops due to compensatory mechanisms
Solution Approach 1:
The patent develops a multi-functional anti-cancer molecule that simultaneously exhibits anti-mitotic and anti-angiogenic activities. The anti-angiogenic component is designed to be broad-spectrum, targeting multiple angiogenic factors rather than a single factor, thereby preventing resistance development through compensatory mechanisms while maintaining reliable anti-angiogenic activity
3Object-affected harmful factors
If antibodies targeting surface molecules are used, then specificity is improved, but production complexity and cost increase
Solution Approach 1:
The patent replaces complex, expensive antibody production with a simpler, more economical synthetic small molecule approach. The small molecule ligand can be synthesized through standard chemical methods, avoiding the lengthy and costly antibody development process while maintaining high specificity for tumour surface nucleolin. This substitution reduces production complexity and cost while preserving targeting specificity
Solution Approach 2:
The invention substitutes the biological antibody system with a chemically synthesized small molecule system. Instead of using complex protein-based antibodies that require sophisticated production facilities, the patent employs a synthetic organic molecule with defined chemical structure that can be produced through conventional chemical synthesis, thereby reducing device complexity and production barriers
4Reliability
If highly hydrophobic anti-cancer molecules are used, then anti-cancer activity is achieved, but bioavailability decreases requiring complicated formulations
Solution Approach 1:
The patent optimizes the physicochemical parameters of the anti-cancer molecule, specifically adjusting the hydrophobicity-hydrophilicity balance. By modifying the molecular structure to achieve appropriate solubility characteristics, the invention improves in vivo bioavailability and pharmacokinetic properties without compromising anti-cancer activity. This parameter optimization eliminates the need for complicated pharmaceutical formulations
Data Source
AI summary
A method for treating disorders involving deregulation of cell proliferation and/or angiogenesis comprising the administration of an effective amount of a multivalent synthetic compound comprising a support on which at least 3 pseudopeptide units are grafted, said compound being of formula (I).