Elastin-Targeting Peptide Composition for Fibrosis Inhibition
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Solution Overview
Problem
Current treatments for organ fibrosis, such as hepatic and pulmonary fibrosis, are inadequate, with existing drugs posing safety risks and being costly, and there is a need for more targeted and effective therapies.
Innovation Solution
A novel peptide compound targeting elastin-derived peptides (EDPs) is designed to inhibit their biological effects, comprising specific amino acid sequences with optional lipophilic substituents, forming linear or cyclic peptides, which are combined with pharmaceutically acceptable carriers for administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If obeticholic acid (OCA) is used to treat fibrosis, then therapeutic effect is improved, but adverse reactions and cost increase
Solution Approach 1:
The patent extracts and targets the specific pathological mechanism of fibrosis by designing a peptide compound that selectively binds to TGF-β1, separating the therapeutic action from the broad-spectrum effects of existing drugs like OCA. This targeted approach eliminates off-target adverse reactions while maintaining anti-fibrotic efficacy.
Solution Approach 2:
The peptide compound acts as an intermediary molecule that specifically mediates the inhibition of TGF-β1 signaling pathway, which is the key driver of fibrosis. This intermediate targeting approach provides more precise control over the therapeutic mechanism, reducing unwanted side effects compared to direct use of OCA.
2Reliability
If obeticholic acid (OCA) is used to treat fibrosis, then therapeutic effect is improved, but treatment cost increases
Solution Approach 1:
The patent employs a peptide-based compound rather than a complex small molecule drug like OCA. Peptides can be synthesized more cost-effectively using solid-phase peptide synthesis methods, making the treatment more economically viable while maintaining therapeutic efficacy.
3Reliability
If natural peptides are used for fibrosis treatment, then basic therapeutic function is provided, but bioactivity and efficacy are limited
Solution Approach 1:
The patent introduces a lipophilic substituent at the N-terminus of the peptide, creating local hydrophobic character that enhances membrane permeability and binding affinity. This localized modification improves the overall bioactivity without altering the core therapeutic function of the peptide sequence.
Solution Approach 2:
The patent modifies physical and chemical parameters of the natural peptide by adding a lipophilic group, which changes the peptide's solubility, membrane interaction, and binding characteristics. These parameter changes result in enhanced bioactivity and therapeutic efficacy.
Data Source
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AI summary
The present invention relates to peptide compound targeting elastin-derived peptides and use thereof. The peptide comprises a parent peptide represented by the following amino acid sequence: R1-Val-Xa2-Gly-Ser-Pro-Ser-Ala-Gln-Xa9-Xa10-Ala-Ser-Pro-Xa14, and is characterized by better biological activity, higher safety and stability, high synthesis yield, low cost, etc. The peptide compound may be used for treating hepatic fibrosis and fibrotic conditions accompanying hepatic disease as well as idiopathic pulmonary fibrosis and fibrotic conditions accompanying pulmonary disease.