hTfR-Binding Peptide for Blood-Brain Barrier Transport
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing methods struggle to effectively deliver high-molecular-weight substances across the blood-brain barrier using transferrin receptor affinity, limiting the ability to target the brain with therapeutic agents.
Innovation Solution
A novel peptide with specific amino acid sequences or modifications that bind to the human transferrin receptor (hTfR), allowing for targeted delivery across the blood-brain barrier.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high-molecular-weight substances are modified to have affinity for the transferrin receptor, then they can pass through the blood-brain barrier, but the complexity of the substance structure increases and manufacturing becomes more difficult
Solution Approach 1:
The invention extracts and utilizes only the essential binding domain of the transferrin receptor (amino acids 739-766) to create a peptide ligand. This extracted peptide sequence (SEQ ID NO: 1) is significantly simpler to manufacture than full transferrin protein while retaining the critical blood-brain barrier penetration capability through specific receptor binding
Solution Approach 2:
The patent employs a short peptide sequence (14 amino acids) instead of large protein molecules. This short peptide is easier to synthesize chemically, more stable, and can be produced at lower cost while maintaining sufficient binding affinity to the transferrin receptor for effective blood-brain barrier transport
2Reliability
If a peptide sequence is designed for strong binding to hTfR, then binding affinity increases, but the peptide structure becomes more complex with multiple amino acid modifications
Solution Approach 1:
The invention focuses modifications on specific local positions within the peptide sequence that are critical for binding. Key modifications include aromatic amino acids at positions 3, 7, and 13, and a basic amino acid at position 12, which locally enhance binding affinity to the transferrin receptor without requiring complex modifications throughout the entire peptide structure
Solution Approach 2:
The patent systematically varies parameters such as amino acid type (aromatic, basic, aliphatic), charge, and hydrophobicity at specific positions to optimize binding affinity. The design explores different combinations of these parameters to achieve strong binding while maintaining a relatively simple overall peptide structure that is feasible to synthesize
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 peptide provides strong binding affinity to hTfR, enabling efficient transport of substances across the blood-brain barrier, facilitating targeted delivery to brain tissues.
Implementation Method 1
a peptide... that binds to the transferrin receptor
Data Source
AI summary
[Problem] To provide: a novel peptide that binds to a human transferrin receptor (hTfR); and various uses of the novel peptide. [Solution] A peptide consisting of an amino acid sequence disclosed in Ala-Val-MeF3C-Val-W7N-Asn-3Py6NH2-F4OMe-Ile-Ile-Arg-Arg-4Py-MeTyr-Cys (SEQ ID NO: 1) or a pharmaceutically acceptable salt thereof; a composite comprising said peptide or pharmaceutically acceptable salt thereof, and a material bound to a linker; a composition comprising said peptide or said composite; and a method for producing a pharmaceutical or diagnostic composition.