Truncated BMP Peptides and Protease Composition for Osteogenesis

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Solution Overview

Problem

Current compositions and methods for using bone morphogenic proteins (BMPs) do not effectively utilize truncated peptides with osteoinductive, chondroinductive, or ligament/tendon differentiating activities, particularly when combined with proteases, to enhance cellular differentiation and growth factor activity.

Innovation Solution

A composition comprising an isolated peptide with an amino acid sequence of 137 residues or less, specifically designed to include at least one protease such as collagenase, dispase, trypsin, or MMP-13, to promote osteogenesis, chondrogenesis, or ligament/tendon differentiation by enhancing the activity of BMPs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If full-length BMPs are used, then osteoinductive and chondroinductive activities are achieved, but the complexity of the protein structure increases manufacturing difficulty

Engineering Contradiction:
Improveosteoinductive activityVSAvoidmanufacturing difficulty
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The BMP protein is divided into functional segments, specifically utilizing truncated peptides (137 residues or less) that contain the essential osteoinductive and chondroinductive domains while removing non-essential portions. This segmentation maintains biological activity while simplifying manufacturing processes

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The essential functional domains are extracted from the full-length BMP protein to create truncated peptides. These extracted peptide sequences (SEQ ID NO: 20-28) retain the core osteoinductive and chondroinductive activities without the complexity of the complete protein structure

Inventive Principle:
Principle #2Taking out (Extraction)

2Ease of manufacture

If truncated BMP peptides are used, then manufacturing complexity is reduced, but growth factor activity may be insufficient without protease enhancement

Engineering Contradiction:
Improvemanufacturing simplicityVSAvoidgrowth factor activity
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

Proteases are introduced as intermediary enzymes that process the truncated BMP peptides to generate fully active growth factors. The proteases cleave the truncated peptides at specific sites to produce mature, bioactive BMP molecules, bridging the gap between simplified peptide structures and full biological activity

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The chemical structure of the truncated peptides is modified through proteolytic processing by added proteases. This parameter change transforms the truncated peptide sequence into the active mature BMP form, enhancing growth factor activity while maintaining manufacturing advantages

Inventive Principle:
Principle #35Parameter changes

3Reliability

If proteases are added to enhance BMP activity, then cellular differentiation is improved, but the composition complexity increases

Engineering Contradiction:
Improvecellular differentiation capabilityVSAvoidcomposition complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The truncated BMP peptides and proteases are combined into a single composition that works synergistically. The proteases process the peptides in situ to generate active BMP, merging the benefits of simplified peptide structure with the activity-enhancing effects of proteolytic processing in one integrated formulation

Inventive Principle:
Principle #5Merging (Combining)

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 combination of truncated BMP peptides with specific proteases significantly increases alkaline phosphatase activity in cells, demonstrating enhanced osteoinductive, chondroinductive, and ligament/tendon differentiating capabilities compared to unmodified BMPs.

Implementation Method 1

A composition comprising an isolated peptide of 137 residues or less... and at least one protease

Methodology Applied
Scientific EffectProteolysis: Hydrolysis

Data Source

PatentEP2751258B1BMP peptides & methods of use
Publication Date: 2019.08.14 LIFENET HEALTH
  • EP2751258B1 patent drawingFigure 1
  • EP2751258B1 patent drawingFigure 2
  • EP2751258B1 patent drawingFigure 3

AI summary

The invention relates to truncated growth factors and variants thereof. The invention also relates to methods of making and using the truncated growth factors. The invention further relates to compositions including a protease and a growth factor comprising a bone morphogenic protein (BMP) or a variant thereof. The invention also relates to methods of using the composition.