Segmented Peptide for Tumor Cell Targeting and Penetration
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Solution Overview
Problem
Current methods for targeting active pharmaceutical ingredients to tumor cells are not selective enough, lacking efficient mechanisms for intracellular delivery and penetration.
Innovation Solution
Development of a polypeptide compound with at least 80% identity to SEQ ID No. 1, 6, or 7, which can modify other pharmaceutical ingredients to enable selective targeting and penetration into neoplastic cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If conventional cell penetration peptides are used, then cell penetration ability is achieved, but selectivity for tumor cells is insufficient
Solution Approach 1:
The invention divides the peptide into two functional domains: a C-terminal domain (residues 1-35) responsible for cell penetration and internalization, and an N-terminal domain (residues 36-50) responsible for tumor cell selectivity through interaction with phosphatidylserine. This segmentation allows each domain to optimize its specific function independently, resolving the contradiction between general penetration ability and tumor-specific selectivity.
Solution Approach 2:
The invention applies local quality by赋予 different functional characteristics to different regions of the peptide. The C-terminal region is optimized for cellular uptake mechanisms, while the N-terminal region is optimized for tumor cell recognition through phosphatidylserine binding. This localized functional differentiation enables simultaneous achievement of penetration and selectivity.
2Reliability
If peptide sequences are modified to improve tumor cell targeting, then selectivity is enhanced, but cell penetration ability may be compromised
Solution Approach 1:
By segmenting the peptide sequence into distinct functional domains, the invention allows the N-terminal region to be optimized for tumor cell targeting while the C-terminal region maintains optimal properties for cell penetration. This prevents the compromise that would occur if the entire peptide sequence were modified uniformly.
Solution Approach 2:
The invention implements local quality by assigning specific functional roles to specific regions: the N-terminal domain handles tumor cell recognition and binding, while the C-terminal domain handles cellular internalization. This localized optimization ensures that modifications for selectivity do not adversely affect penetration ability.
3Ease of manufacture
If the peptide structure is simplified, then manufacturing is easier, but functional specificity is reduced
Solution Approach 1:
The invention segments the 50-residue peptide into two functional domains with distinct roles. This segmentation allows for modular synthesis strategies where each domain can be optimized independently for both manufacturing efficiency and functional specificity, resolving the contradiction between synthesis simplicity and functional precision.
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 compound effectively internalizes into tumor cells, facilitating the delivery of modified pharmaceutical ingredients, thereby enhancing cancer diagnosis, prognosis, and treatment.
Implementation Method 1
CPPs typically do not exceed 30 residues in length and generally carry a positive charge, which facilitates electrostatic interactions with the negatively charged cell surface
Implementation Method 2
The mechanism of action of Amblyomin-X involves inhibition of the proteasome, which occurs preferentially through the trypsin-like (T-L) activity of the proteasome
Implementation Method 3
The recombinant protein form of Amblyomin-X showed antitumor activity via apoptosis induction and proteasome inhibition
Implementation Method 4
Amblyomin-X induces ER stress, mitochondrial dysfunction, and caspase activation in human melanoma and pancreatic tumor cell
Implementation Method 5
The compound of the invention effectively internalizes into tumor cells, facilitating the delivery of modified pharmaceutical ingredients
Data Source
AI summary
The invention pertains to the technical fields of pharmaceutical sciences, immunology, diagnosis and/or treatment of cancer. Specifically, the invention relates to peptides derived from the C-terminal portion of the tick amblyomin-X protein, said peptides being intended for targeting or promoting the internalization of molecular entities into the intracellular domain of eukaryotic or neoplastic cells. The invention also relates to the use of said peptides for modifying other pharmaceutically active ingredients, to a pharmaceutical composition comprising said peptides and to a method of diagnosis, prognosis and/or treatment of cancer or other cell-altering conditions.