Brain Tumor-Targeting Peptide for Blood-Brain Barrier Delivery

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Solution Overview

Problem

Current therapeutic drugs for brain tumors are limited by the blood-brain barrier, making it difficult for most drugs to effectively target brain tumors.

Innovation Solution

A brain tumor targeted molecule is developed, comprising a blood-brain barrier crossing region and a tumor target region, where the blood-brain barrier crossing region includes the peptide sequence TFYGGRPKRNNFLRGIRSRGD, and the tumor target region can include sequences such as CGKRK or ATWLLPPR, allowing the molecule to efficiently cross the blood-brain barrier and target brain tumors.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional therapeutic drugs are used for brain tumors, then the drugs have limited effectiveness, but the blood-brain barrier prevents most substances from entering the brain

Engineering Contradiction:
Improvedrug effectivenessVSAvoidblood-brain barrier blocking
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses a peptide vector as an intermediary carrier to transport therapeutic drugs across the blood-brain barrier. The peptide sequence TFYGGRPKRNNFLRGIRSRGD acts as a mediator that facilitates drug entry into the brain by interacting with transport mechanisms in the blood-brain barrier, thereby enabling drugs that would otherwise be blocked to reach their target effectively

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite structure combining the peptide vector with therapeutic drugs. This composite material allows the drug to be delivered through the blood-brain barrier while maintaining its therapeutic function, resolving the contradiction between barrier protection and drug delivery

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If RGD peptide is used to cross the blood-brain barrier, then the peptide can reach brain tumors, but the ability to specifically target tumor cells must be maintained

Engineering Contradiction:
Improveblood-brain barrier crossing abilityVSAvoidtumor targeting specificity
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent merges two functional peptide sequences into one: the blood-brain barrier crossing sequence TFYGGRPKRNNFLRGIR and the tumor-targeting RGD sequence. This combined peptide simultaneously performs both functions - crossing the blood-brain barrier and specifically binding to integrins on tumor cells, thus resolving the contradiction between barrier penetration and targeting specificity

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The designed peptide vector possesses multiple functions: it can cross the blood-brain barrier, target tumor cells specifically through RGD-integrin interaction, and serve as a carrier for therapeutic drugs. This multi-functionality allows a single molecule to address multiple requirements that would otherwise be in conflict

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 brain tumor targeted molecule effectively crosses the blood-brain barrier and retains its ability to target brain tumors, providing a new platform for both diagnostic imaging and targeted therapy of brain tumors.

Implementation Method 1

based on the idea of receptor-mediated pathway, the receptor pathway mediated by receptor LRP1 can be used to select a skeleton

Methodology Applied
Scientific EffectReceptor-mediated transport:

Implementation Method 2

RGD is a short peptide sequence containing arginine-glycine-aspartic acid (Arg-Gly-Asp), which acts as a recognition site for the interaction of integrins and its ligands

Methodology Applied
Scientific EffectMolecular recognition and binding:

Data Source

PatentUS12343400B2Brain tumor-targeting peptide and application thereof
Publication Date: 2025.07.01 JIANGSU JITRI MOLECULAR ENG INST CO LTD
  • US12343400B2 patent drawing
  • US12343400B2 patent drawing
  • US12343400B2 patent drawing

AI summary

The present invention related to a brain tumor-targeting peptide, a coding nucleic acid thereof, and a vector and host cell comprising the coding nucleic acid. The targeting peptide linked to a diagnostic marker can be used in brain tumor diagnosis, especially in brain tumor imaging; and the targeting peptide when linked to a therapeutic drug can carry the drug directly to a brain tumor lesion so as to achieve brain tumor treatment.