Modified aFGF Peptide Stability via N-Terminal Deletion

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Solution Overview

Problem

Native human acidic fibroblast growth factor (aFGF) peptides have stability issues due to their similarity with interleukin-1, leading to immuno-response activation and structural instability, which affects their therapeutic applications.

Innovation Solution

A modified peptide, aFGF135, is developed by deleting 20 amino acids from the N-terminal of native human aFGF and adding Alanine, resulting in a more stable sequence with improved thermal stability and distinct structural characterization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If native human aFGF is used, then biological activity is maintained, but stability is poor due to immuno-response activation and structural instability

Engineering Contradiction:
ImprovestabilityVSAvoidamino acid sequence complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts and removes the problematic N-terminal 20 amino acids from native human aFGF that cause immuno-response activation and structural instability. This extraction eliminates the harmful similarity with interleukin-1 while preserving the core biological activity of the remaining 135 amino acids.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent modifies only the specific N-terminal region of the aFGF molecule where the problem originates, rather than changing the entire structure. The modification is localized to deleting residues 1-20 and adding Alanine at position 1, preserving the functional integrity of the C-terminal region while improving overall stability.

Inventive Principle:
Principle #3Local quality

2Reliability

If N-terminal 20 amino acids are deleted and Alanine is added, then stability is improved, but sequence similarity with native aFGF is reduced

Engineering Contradiction:
Improvethermal stabilityVSAvoidsequence fidelity
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent changes the physical-chemical parameters of the N-terminal region by deleting 20 amino acids and adding a single Alanine residue. This parameter change fundamentally alters the thermal stability and immuno-genicity of the peptide while maintaining the core functional structure.

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If native aFGF structure is preserved, then receptor binding capability is maintained, but resistance to denaturation and hydrolysis is insufficient

Engineering Contradiction:
Improveresistance to denaturation and hydrolysisVSAvoidstructural composition
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent applies preliminary anti-action by pre-modifying the N-terminal structure to prevent future denaturation and hydrolysis. The deletion of unstable N-terminal residues and addition of Alanine creates a more resistant structure that proactively defends against thermal and enzymatic degradation before damage occurs.

Inventive Principle:
Principle #9Preliminary anti-action

Data Source

PatentEP2338909B1Modified peptide of human acidic fibroblast growth factor
Publication Date: 2013.07.10 EU SOL BIOTECH
  • EP2338909B1 patent drawingFigure 1
  • EP2338909B1 patent drawingFigure 2A
  • EP2338909B1 patent drawingFigure 2B

AI summary

An modified peptide of human acidic fibroblast growth factor (aFGF), comprising a native human aFGF shortened by a deletion of a deletion of 20 amino acids from N-terminal of the native human aFGF, and an addition of Alanine (Ala) before the shortened native aFGF is provided.