Fused Polypeptide Targeting Multiple Fibrosis Pathways With Reduced Toxicity
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Solution Overview
Problem
Existing drugs for treating fibrosis, such as pulmonary, hepatic, renal, myocardial, and skin fibrosis, suffer from high toxicity, low safety, and single pharmacological actions.
Innovation Solution
A fused polypeptide with multifunctional activities targeting angiogenesis, integrins, and matrix metalloproteinases is designed to inhibit fibrosis by reducing fibroblast activation and extracellular matrix deposition, comprising specific amino acid sequences like Pro-Arg-Cys-X-Y-Gly-Glu-Gly-Gly-Gly-Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Val-Pro-Gly-Gly-Gly-Arg-Gly-Asp, where X and Y can be Trp or Tyr.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing drugs for treating fibrosis are used, then fibrosis treatment is achieved, but high toxicity and low safety occur
Solution Approach 1:
The patent applies composite materials by fusing multiple functional domains into a single polypeptide molecule. The fused polypeptide comprises an MMP inhibitor domain, an angiogenesis inhibitor domain, and an integrin inhibitor domain, creating a composite therapeutic agent that combines multiple pharmacological activities. This composite structure allows simultaneous targeting of multiple fibrosis pathways while maintaining safety, as the polypeptide uses natural amino acid sequences without obvious toxic or side effects.
Solution Approach 2:
The patent implements universality by designing a multifunctional polypeptide that can treat various types of fibrosis (pulmonary, hepatic, renal, myocardial, and skin fibrosis) through multiple mechanisms. The single polypeptide molecule performs multiple functions: inhibiting MMPs to reduce ECM degradation, inhibiting angiogenesis to prevent new blood vessel formation, and inhibiting integrins to block fibroblast activation. This multi-functional approach eliminates the need for multiple separate drugs and reduces overall toxicity.
2Reliability
If existing fibrosis drugs are used, then treatment effect is achieved, but single pharmacological actions limit efficacy
Solution Approach 1:
The patent directly addresses this contradiction by creating a polypeptide with three distinct inhibitory functions. The MMP inhibitor domain targets matrix metalloproteinases to prevent ECM breakdown, the angiogenesis inhibitor domain blocks VEGF signaling to prevent new vessel formation, and the integrin inhibitor domain prevents fibroblast activation and ECM deposition. This multi-pharmacological action significantly enhances treatment efficacy compared to single-action drugs.
Solution Approach 2:
The fused polypeptide combines multiple pharmacological domains into one molecule, creating a composite therapeutic agent that simultaneously targets multiple pathways involved in fibrosis. This composite structure enables the drug to address the complexity of fibrosis pathogenesis through coordinated inhibition of MMPs, angiogenesis, and integrin signaling, thereby achieving superior treatment efficacy.
3Adaptability or versatility
If multiple drugs are used to target multiple fibrosis pathways, then treatment coverage improves, but device complexity and administration burden increase
Solution Approach 1:
The patent merges multiple separate therapeutic agents into a single fused polypeptide molecule. Instead of administering separate drugs for MMP inhibition, angiogenesis inhibition, and integrin inhibition, the patent combines all three functional domains into one polypeptide that can be administered as a single agent. This merging simplifies the drug regimen while maintaining comprehensive treatment coverage across multiple fibrosis pathways.
Solution Approach 2:
The multifunctional polypeptide serves as a universal treatment agent that can address various types of fibrosis (pulmonary, hepatic, renal, myocardial, skin) through its multiple inhibitory domains. This single universal agent replaces the need for multiple specialized drugs, reducing administration burden while maintaining broad treatment coverage across different fibrosis conditions.
Data Source
AI summary
The present disclosure discloses use of a fused polypeptide with multifunctional activities. In the fused polypeptide with multifunctional activities, the polypeptide contains the following domains: Pro-Arg-Cys-X-Y-Gly-Glu, where X is Trp or Tyr, and Y is Arg or Cys; and Gly-Gly-Gly-Gly-Ile-Val-Arg-Arg-Ala-Asp-Arg-Ala-Ala-Val-Pro-Gly-Gly-Gly-Gly-Arg-Gly-Asp; or a sequence of any amino acid mutated in the foregoing domains. The fused polypeptide can be used for treating various fibrosis diseases and symptoms, including pulmonary fibrosis, hepatic fibrosis, skin fibrosis, renal fibrosis, myocardial fibrosis, and lung tissue lesions.