Peptidomimetic NKB Antagonists for Fish Maturation Control

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Solution Overview

Problem

Current technologies lack NKB antagonists specifically designed for fish, which are needed to delay or inhibit fish maturation and control reproductive parameters, unlike existing NKB agonists that advance puberty and stimulate reproduction.

Innovation Solution

Development of peptidomimetic NKB and NKF antagonists, such as those following the Formula I: X1-NMeVal-X4-Leu-Met-Z, which alter specific amino acid residues to change activity from agonistic to antagonistic, inhibiting tac-3 receptor activity and used in pharmaceutical or food compositions to delay fish maturation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If NKB agonists are used to advance puberty and stimulate reproduction, then reproductive activity is improved, but maturation timing cannot be delayed

Engineering Contradiction:
Improvereproductive activityVSAvoidmaturation timing
Core Design Contradiction:
ProductivityVSLoss of time

Solution Approach 1:

The patent applies inversion by developing antagonists that block NKB receptor activity instead of using agonists that stimulate it. The peptidomimetic compounds (Formula I) with specific amino acid sequences at positions X1, X2, X3, and X4 bind to tac3 receptors and prevent NKB from activating them, thereby delaying maturation while maintaining reproductive capability when needed.

Inventive Principle:
Principle #13The other way round (Inversion)

2Loss of time

If existing NKB antagonists are used in fish, then maturation can be delayed, but they are not specifically designed for fish reproduction control

Engineering Contradiction:
Improvematuration timingVSAvoidspecificity for fish
Core Design Contradiction:
Loss of timeVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by designing peptidomimetic compounds with specific amino acid sequences tailored to fish tac3 receptors. The compounds include specific residues at positions X1, X2, X3, and X4 that are optimized for binding to fish NKB receptors, ensuring high specificity and effectiveness in fish reproduction control rather than using generic mammalian antagonists.

Inventive Principle:
Principle #3Local quality

3Productivity

If peptidomimetic NKB antagonists are developed, then fish maturation can be delayed with increased growth rates, but compound complexity increases

Engineering Contradiction:
Improvegrowth rateVSAvoidcompound structure
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying amino acid residues at specific positions (X1, X2, X3, X4) in the peptidomimetic sequence to optimize both binding affinity and growth promotion. By modifying these key parameters in the peptide structure, the compounds achieve delayed maturation and increased growth rates while maintaining manageable structural complexity through defined sequence patterns.

Inventive Principle:
Principle #35Parameter changes

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 NKB antagonists effectively delay or inhibit fish maturation, allowing for increased growth rates and altered sex determination, demonstrated through in-vitro and in-vivo experiments showing reduced gonadotropin release and histological changes in fish gonads.

Implementation Method 1

inhibiting tac-3 receptor activity in fish by NKB antagonists can delay or inhibit maturation and reproduction

Methodology Applied
Scientific EffectReceptor binding inhibition:

Data Source

PatentUS10155790B2Antagonists of neurokinin B in fish reproduction
Publication Date: 2018.12.18 YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD
  • US10155790B2 patent drawing
  • US10155790B2 patent drawing
  • US10155790B2 patent drawing

AI summary

Provided are Peptide-based neurokinin antagonists of fish reproduction. Compositions including antagonists of fish neurokinin and methods of inhibiting or delaying puberty, fish maturation or reproduction processes using these compounds are also provided.