Cyclic Peptide Angiogenic Agent for Tissue Regeneration
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Solution Overview
Problem
Existing peptide-based angiogenic agents have limited persistence due to rapid degradation in the body, resulting in weak angiogenic effects, which is a challenge for effective tissue compatibility and regeneration in ischemic disease treatments and organ transplantation.
Innovation Solution
A novel compound with a modified structure, including cyclic peptides with oxyethylene units and specific amino acid sequences, is designed to resist endogenous enzymes, enhancing its persistence and angiogenic activity, thereby improving tissue compatibility and regeneration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a peptide-based angiogenic agent is used, then safety is improved due to metabolism into amino acids, but persistence and angiogenic effect are worsened due to rapid degradation
Solution Approach 1:
The patent modifies the peptide structure by incorporating non-natural amino acids and cyclic structures to change the chemical parameters of the molecule, making it resistant to enzymatic degradation while maintaining its biological activity. This resolves the contradiction by preserving safety through controlled modification while dramatically improving persistence.
Solution Approach 2:
The invention creates a composite peptide structure combining natural amino acids with non-natural amino acid residues and cyclic modifications. This composite approach allows the molecule to retain biocompatibility and safety while gaining resistance to degradation, thus improving persistence without sacrificing safety.
2Strength
If conventional biomaterials like apatite or titanium are used, then structural support is provided, but tissue compatibility and engraftment are worsened due to poor compatibility with surrounding tissues
Solution Approach 1:
The patent combines structural biomaterials (apatite or titanium) with the novel angiogenic peptide compound. This merging allows the structural material to provide mechanical support while the peptide component actively promotes angiogenesis and tissue compatibility, resolving the contradiction between strength and biocompatibility.
Solution Approach 2:
The angiogenic peptide acts as an intermediary substance that mediates between the inert structural biomaterial and the surrounding living tissue. It facilitates communication and interaction, promoting vascularization and tissue integration around the implant, thus improving compatibility without compromising structural integrity.
3Duration of action of moving object
If NGF or bFGF are used for angiogenesis, then some angiogenic effect is achieved, but safety is worsened due to malignant transformation or infiltration
Solution Approach 1:
The patent designs a peptide-based angiogenic agent that is metabolized into amino acids, making it a temporary, biodegradable therapeutic. This approach provides sufficient angiogenic effect during the critical period needed while avoiding the long-term safety risks of growth factors that can cause malignant transformation. The agent performs its function and then safely degrades.
Solution Approach 2:
By modifying the peptide structure with non-natural amino acids and cyclic modifications, the invention changes the parameters of angiogenic stimulation to be more controlled and localized. This prevents the uncontrolled proliferation and malignant transformation associated with conventional growth factors like NGF and bFGF, while maintaining effective angiogenesis.
Data Source
AI summary
Disclosed are a novel compound having a higher angiogenic effect than that of a known peptide-based angiogenic agent, and an angiogenic agent including the novel compound. The compound is represented by the following formula [1]: Cyclic(Cys-O2Oc-SVV(F/Y)GLRG-Cys)-NH2 (wherein the number of oxyethylene units, represented by O2Oc, is within the range of 2 to 6), the following formula [II]: Cyclic(O2Oc-SVV(F/Y)GLRQ)-NH2 [II] (wherein the number of oxyethylene units, represented by O2Oc, is within the range of 2 to 6), or the following formula [III]: O2Oc-SVV(F/Y)GLR-NH2 [III] (wherein the number of oxyethylene units, represented by O2Oc, is within the range of 2 to 6).