Mini-hepcidin Peptides for Iron Overload Treatment

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Solution Overview

Problem

Current treatments for iron overload diseases such as hereditary hemochromatosis and iron-loading anemias are burdensome and often ineffective, with regular phlebotomy being the only option for hemochromatosis and iron chelation showing frequent side effects and limited efficacy.

Innovation Solution

Development of peptides that mimic hepcidin activity by binding to ferroportin, inducing its internalization and degradation, thereby regulating iron levels, including specific peptide structures and modifications that enhance activity and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If regular phlebotomy is used to treat hereditary hemochromatosis, then iron overload is reduced, but the treatment is very burdensome for patients

Engineering Contradiction:
Improveeffectiveness of iron overload treatmentVSAvoidburden on patient
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent creates mini-hepcidin peptides (copies of the natural hepcidin hormone) that replicate its iron-regulatory function. These synthetic peptides bind to ferroportin and induce its internalization and degradation, thereby reducing iron overload without requiring repeated phlebotomy procedures. This copying approach provides a pharmacological alternative that is less burdensome while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #26Copying

2Reliability

If iron chelation is used to treat iron-loading anemias, then iron overload is reduced, but the treatment is very burdensome, sometimes ineffective and accompanied by frequent side effects

Engineering Contradiction:
Improveeffectiveness of iron overload treatmentVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The mini-hepcidin peptides replicate the natural hepcidin mechanism of action by binding to ferroportin and inducing its degradation. This approach mimics the body's natural iron regulation system rather than using external chelating agents, thereby achieving iron reduction without the side effects associated with iron chelation therapy.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The hepcidin peptide therapy leverages the body's own iron regulatory pathways. By administering hepcidin peptides that naturally bind to ferroportin and trigger its internalization, the treatment uses the body's inherent mechanisms to eliminate excess iron, avoiding the need for exogenous chelating substances that cause side effects.

Inventive Principle:
Principle #25Self-service

3Length of moving object

If the N-terminal region of hepcidin is deleted to create shorter peptides, then peptide length is reduced, but iron-regulatory function is lost

Engineering Contradiction:
Improvepeptide lengthVSAvoidiron-regulatory function
Core Design Contradiction:
Length of moving objectVSReliability

Solution Approach 1:

The patent segments the full-length hepcidin peptide to identify the minimal functional unit required for iron regulation. Through systematic deletion studies, the invention determined that residues 3-10 (Hep3-10) constitute the essential N-terminal segment that retains bioactivity. This segmentation approach identifies the critical functional domain while removing non-essential portions.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention extracts the essential N-terminal segment (residues 3-10) from the full-length hepcidin peptide to create a mini-hepcidin that retains iron-regulatory function. This extracted segment contains the critical amino acids necessary for ferroportin binding and internalization, while eliminating the need for the complete 25-residue sequence.

Inventive Principle:
Principle #2Taking out (Extraction)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The peptides effectively lower plasma iron concentrations, providing a potential therapeutic alternative to existing treatments by mimicking hepcidin activity, thus addressing the limitations of current treatments for iron overload diseases.

Implementation Method 1

Hepcidin acts by binding to its receptor, the iron export channel ferroportin, and causing its internalization and degradation

Methodology Applied
Scientific EffectProtein degradation:

Data Source

PatentEP3208279B1MINI-hepcidin peptides and methods of using thereof
Publication Date: 2021.04.21 RGT UNIV OF CALIFORNIA
  • EP3208279B1 patent drawingFigure 1~2B
  • EP3208279B1 patent drawingFigure 3A~3B
  • EP3208279B1 patent drawingFigure 3C~4

AI summary

Disclosed herein are peptides which exhibit hepcidin activity and methods of making and using thereof.