Recombinant Peptide Stability via Segmented Tripeptide Core

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Solution Overview

Problem

Current methods for producing peptides, particularly for reproductive and sexual function stimulation, are costly and inefficient due to multistage synthesis and susceptibility to proteolysis, leading to reduced efficacy and prolonged treatment durations.

Innovation Solution

Development of peptides with the general formula A-Thr-Lys-Pro-B-C-D-X, where specific amino acid residues are selected based on bioinformatic analysis to enhance stability and activity, focusing on the Thr-Lys-Pro tripeptide as a core molecule, and synthesizing tetrapeptides and higher peptides to maintain reproductive and sexual function stimulating activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional multistage synthesis methods are used to produce peptides, then peptide production is achieved, but the production cost increases and treatment duration is prolonged

Engineering Contradiction:
Improvepeptide production efficiencyVSAvoidtreatment duration
Core Design Contradiction:
ProductivityVSLoss of time

Solution Approach 1:

The peptide structure is segmented into a core stable tripeptide (Thr-Lys-Pro) and variable terminal residues. This segmentation allows the core structure to provide stability and resistance to proteolysis, while the terminal residues can be optimized for specific biological activities, thereby improving production efficiency and reducing treatment duration

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention changes the structural parameters of peptides by establishing a specific general formula with constrained amino acid positions. This parameter optimization ensures resistance to proteolysis and enhances reproductive and sexual function stimulating activity, leading to reduced treatment duration and improved productivity

Inventive Principle:
Principle #35Parameter changes

2Productivity

If conventional peptide synthesis methods are used, then peptide production is achieved, but production costs increase

Engineering Contradiction:
Improvepeptide production efficiencyVSAvoidproduction cost
Core Design Contradiction:
ProductivityVSEase of manufacture

Solution Approach 1:

By optimizing the amino acid sequence parameters according to the general formula, the invention achieves enhanced stability and activity, which reduces the need for complex purification steps and lowers production costs while maintaining high productivity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The peptide structure combines a stable core tripeptide (Thr-Lys-Pro) with variable terminal residues, creating a composite structure that provides both stability and specific biological activity. This composite approach improves manufacturing efficiency and reduces costs

Inventive Principle:
Principle #40Composite materials

3Reliability

If peptides are used for treatment, then reproductive and sexual function stimulation is achieved, but susceptibility to proteolysis reduces efficacy

Engineering Contradiction:
Improvepeptide efficacyVSAvoidresistance to proteolysis
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention applies local quality by providing different functional characteristics to different parts of the peptide molecule. The core Thr-Lys-Pro tripeptide provides stability and resistance to proteolysis, while the terminal residues provide specific biological activity, thereby achieving both reliability and stability

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The peptide structure combines a stable core tripeptide (Thr-Lys-Pro) with variable terminal residues, creating a composite structure that provides both stability and specific biological activity. This composite approach improves manufacturing efficiency and reduces costs

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3650457B1Method for producing a recombinant peptide and resultant peptide
Publication Date: 2021.03.17 OVB (IRELAND) LTD
  • EP3650457B1 patent drawingFigure 1~2
  • EP3650457B1 patent drawingFigure 3
  • EP3650457B1 patent drawingFigure 4~5

AI summary

The invention provides a peptide of formula Thr-Lys-Pro-Arg- Pro-Phe-X, wherein X is OH, OCH3, or NH2 group, that is useful in stimulating sexual or reproductive function.