Anticancer Peptides Targeting Pancreatic Cancer Cells
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Solution Overview
Problem
Current treatments for pancreatic cancer are ineffective, with limited therapeutic options and high mortality rates due to late detection and resistance to traditional chemotherapy, highlighting the need for novel anticancer agents that are specific, stable, and non-toxic.
Innovation Solution
Development of peptides with a cysteine residue at the terminal end, which exhibit high solubility, stability, and specificity for cancer cells, allowing for targeted inhibition of cancer growth without toxic side effects, formulated into pharmaceutical compositions for therapeutic use.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional chemotherapy is used for pancreatic cancer treatment, then cancer cells are targeted for destruction, but severe toxic side effects and multidrug resistance occur
Solution Approach 1:
The patent modifies the chemical structure of peptide therapeutics by incorporating specific amino acid sequences and post-translational modifications (such as N-terminal acetylation and C-terminal amidation) to enhance cancer selectivity and reduce toxic effects on normal cells
Solution Approach 2:
The invention uses small peptide molecules (rather than large proteins or antibodies) that are easily synthesized, rapidly degraded by the body, and do not accumulate in organs, thereby minimizing long-term toxic effects while maintaining therapeutic activity
2Reliability
If surgical resection is performed for pancreatic cancer, then curative treatment is achieved, but only 10-25% of patients are candidates due to late detection
Solution Approach 1:
The patent employs peptide therapeutics as intermediary agents that can be administered systemically to target cancer cells at early stages, potentially enabling earlier intervention before metastasis occurs, thereby increasing the proportion of patients eligible for curative treatment
3Reliability
If peptide therapeutics are used for cancer treatment, then high activity and specificity are achieved, but low stability and protease resistance hinder clinical development
Solution Approach 1:
The patent enhances peptide stability by modifying structural parameters including N-terminal acetylation, C-terminal amidation, and incorporation of protease-resistant amino acid sequences, thereby improving half-life and reducing degradation while maintaining cancer inhibitory activity
Solution Approach 2:
The invention creates composite peptide structures combining multiple functional elements (cell-penetrating domains, cancer-targeting sequences, and stability-enhancing modifications) to achieve both high efficacy and improved pharmacokinetic properties
4Reliability
If recombinant antibodies or proteins are used for cancer treatment, then therapeutic effect is achieved, but high immunogenicity and complexity are present
Solution Approach 1:
The patent employs small peptide molecules (8-20 amino acids) that are significantly simpler to synthesize than recombinant antibodies or proteins, can be produced by conventional chemical synthesis methods, and elicit minimal immunogenic responses while maintaining therapeutic efficacy
Solution Approach 2:
The invention extracts and utilizes only the essential functional elements of larger protein therapeutics (specifically the cancer-targeting and cell-penetrating functions) in the form of short peptide sequences, eliminating unnecessary complexity and reducing immunogenicity
Data Source
Figure 1A~1B
Figure 2
AI summary
The present invention provides a peptide of formula (I), or a pharmaceutically acceptable salt thereof, wherein the N-terminal group of the peptide is a monoradical of formula - NHR1; the C-terminal group of the peptide is a monoradical of formula -C(O)-R2; R1 is a monoradical selected from hydrogen and -C(O)-(C1-C20)alkyl; R2 is a monoradical selected from -OH and -NR3R4 radical; R3 and R4 are independently selected from hydrogen and (C1-C10)alkyl; "a" to "j" are integers from 0 to 1, provided that at least one of "a" to "j" is 1; and X1 represents any amino acid. The present invention also provides conjugates and compositions comprising the peptide of formula (I).