Multimeric Peptide Vectors for Blood-Brain Barrier Transport
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Solution Overview
Problem
The blood-brain barrier (BBB) restricts the entry of therapeutic agents, including peptides and proteins, into the brain, limiting the treatment of central nervous system (CNS) disorders due to its selective permeability to small, lipophilic molecules.
Innovation Solution
Development of dimeric or multimeric peptide vectors that can efficiently cross the BBB and target specific cell types, such as liver, lung, spleen, and muscle, when conjugated with therapeutic agents, enhancing their transport and delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide and protein therapeutics are used to treat CNS disorders, then therapeutic efficacy is improved, but BBB permeability is poor
Solution Approach 1:
The patent merges a peptide vector (Angiopep-2) with a therapeutic agent to form a conjugate. The peptide vector component facilitates BBB crossing while the therapeutic agent provides the desired pharmacological effect, thus combining the advantages of both components to overcome the permeability barrier.
Solution Approach 2:
The peptide vector acts as an intermediary carrier that mediates the transport of the therapeutic agent across the BBB. It interacts with BBB transport mechanisms to enable the passage of the conjugate, effectively serving as a bridge between the blood and brain compartments.
2Object-affected harmful factors
If only small lipophilic molecules are used to cross BBB, then permeability is improved, but therapeutic efficacy for CNS disorders is limited
Solution Approach 1:
The peptide vector serves as an intermediary that enables larger, more hydrophilic therapeutic agents to cross the BBB by utilizing BBB transport mechanisms, thereby overcoming the size and hydrophobicity limitations of conventional small lipophilic molecules.
Solution Approach 2:
The invention changes the parameters of the therapeutic agent by conjugating it to a peptide vector, effectively altering its size, hydrophobicity, and transport properties to enable BBB penetration while maintaining therapeutic activity.
3Productivity
If multimeric peptide vectors are conjugated to therapeutic agents, then transport efficiency across BBB is improved, but compound complexity increases
Solution Approach 1:
The invention segments the therapeutic agent into a conjugate structure where the peptide vector and therapeutic agent are linked through a linker. This segmentation allows the peptide vector to independently facilitate transport while the therapeutic agent retains its pharmacological function, improving transport efficiency without excessive complexity.
Solution Approach 2:
The linker acts as an intermediary connection between the peptide vector and therapeutic agent, providing a stable yet flexible bond that maintains the functional integrity of both components while enabling efficient transport across the BBB.
Data Source
AI summary
The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.