GIP Peptide Modulation of Synaptic LTP for Cognitive Disorders

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Solution Overview

Problem

Current treatments fail to effectively prevent or reverse diminished cognitive function associated with impaired long-term potentiation (LTP) of synaptic transmission, which is linked to various neurological disorders, including age-related memory impairment and neurodegenerative diseases like Alzheimer's.

Innovation Solution

The use of peptides comprising at least 12 amino acid residues from the N-terminal end of gastric inhibitory polypeptide (GIP) or its analogues, administered to enhance or impair LTP as needed, to treat and prophylaxis neurological disorders related to dysfunctional synaptic transmission.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for neurological disorders with impaired LTP, then current standard therapies are applied, but cognitive function remains diminished and treatment effectiveness is insufficient

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidcognitive function

Core Design Contradiction:

ReliabilityVSLoss of information

Solution Approach 1:

The patent changes the chemical parameter by using GIP peptide analogues with specific amino acid sequences (at least 12 residues from N-terminal end) that bind to GIP receptors in the brain, thereby modulating LTP and improving cognitive function in neurological disorders

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The GIP peptide acts as an intermediary substance that mediates between the external environment and the brain's synaptic transmission system, binding to GIP receptors to restore or enhance LTP and improve cognitive function

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If GIP peptide analogues are administered to enhance LTP, then cognitive deficits are improved, but the complexity of peptide administration and formulation increases

Engineering Contradiction:

Improvecognitive function improvementVSAvoidpeptide administration system

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the GIP peptide into functional regions (N-terminal end with at least 12 amino acid residues) that are critical for LTP enhancement, allowing for optimized peptide design and administration

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent modifies peptide parameters such as amino acid sequence, length (at least 12 residues), and structural analogues to optimize binding affinity and LTP enhancement while controlling administration complexity

Inventive Principle:

Principle #35Parameter changes

3Reliability

If GIP peptides are used to treat disorders with overactive cognitive processes, then elevated LTP is reduced, but the risk of affecting normal cognitive function increases

Engineering Contradiction:

Improvecognitive process regulationVSAvoidcognitive function disruption

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent enables dynamic regulation of LTP by administering GIP peptide analogues that can enhance or impair LTP depending on the specific neurological disorder, allowing flexible adaptation to different clinical needs

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The patent utilizes parameter changes in peptide structure and administration dosage to achieve selective modulation of LTP, enhancing it for cognitive deficits while controlling it for overactive processes, thereby minimizing harmful effects

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

These peptides effectively modulate LTP, enhancing it to treat cognitive deficits and potentially delaying the onset of impaired cognitive processes, while also serving as a therapeutic measure for disorders with overactive cognitive processes by reducing elevated LTP levels.

Implementation Method 1

GIP acts on GIP receptors in the brain to modulate long-term potentiation (LTP) of synaptic transmission

Methodology Applied

Scientific EffectReceptor binding:

Implementation Method 2

The peptide acts on GIP receptors in the brain to modulate long-term potentiation (LTP) of synaptic transmission, enhancing it to treat cognitive deficits

Methodology Applied

Scientific EffectSynaptic transmission modulation:

Data Source

PatentUS9062125B2Use of GIP for the treatment of disorders associated with dysfunctional synaptic transmission

Publication Date: 2015.06.23 INNOVATION ULSTER LTD

AI summary

The present invention relates to a peptide comprising at least 12 amino acid residues from the N-terminal end of gastric inhibitory polypeptide, or an analog thereof, which are useful to prophylactically prevent, improve, or reverse the diminished cognitive function associated with these types of disorders, by increasing (or sustaining) the LTP of synaptic transmission. Moreover, sustaining LTP may find utility in the prophylaxis of neurological disease by delaying the onset of impaired cognitive processes, and could serve as a treatment, not only for the diminished cognitive function caused by neurodegeneration, but also for the dysfunctional cognitive processes associated with trauma or age. Additionally, the peptides and analogs of the present invention find are useful to improve the altered cognitive function associated with hyperexcitability-type disorders, by reducing the elevated level of LTP of synaptic transmission.