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Novel peptides functionally targeting in vivo human lung cancer discovered by in vivo peptide displayed phage
Kyoung Jin Lee1, Jae Hee Lee, Hye Kyung Chung
1Institute for Innovative Cancer Research, ASAN Medical Center, University of Ulsan College of Medicine, Seoul, 138-736, Korea.
Abstract:
Discovery of the cancer-specific peptidic ligands have been emphasized for active targeting drug delivery system and non-invasive imaging. For the discovery of useful and applicable peptidic ligands, in vivo peptide-displayed phage screening has been performed in this study using a xenograft mouse model as a mimic microenvironment to tumor. To seek human lung cancer-specific peptides, M13 phage library displaying 2.9 × 10(9) random peptides was intravenously injected into mouse model bearing A549-derived xenograft tumor through the tail vein. Then the phages emerged from a course of four rounds of biopanning in the xenograft tumor tissue. Novel peptides were categorized into four groups according to a sequence-homology phylogenicity, and in vivo tumor-targeting capacity of these peptides was validated by whole body imaging with Cy5.5-labeled phages in various cancer types. The result revealed that novel peptides accumulated only in adenocarcinoma lung cancer cell-derived xenograft tissue. For further confirmation of the specific targeting ability, in vitro cell-binding assay and immunohistochemistry in vivo tumor tissue were performed with a selected peptide. The peptide was found to bind intensely to lung cancer cells both in vitro and in vivo, which was efficiently compromised with unlabeled phages in an in vitro competition assay. In conclusion, the peptides specifically targeting human lung cancer were discovered in this study, which is warranted to provide substantive feasibilities for drug delivery and imaging in terms of a novel targeted therapeutics and diagnostics.
Insights
Researchers discovered novel peptides that specifically target human lung cancer. These peptides show potential for advanced drug delivery systems and non-invasive imaging, offering new avenues for targeted cancer therapeutics and diagnostics.
Area of Science:
- Oncology
- Molecular Biology
- Biotechnology
Background:
- Cancer-specific peptidic ligands are crucial for targeted drug delivery and imaging.
- In vivo screening methods are essential for discovering effective cancer-targeting ligands.
Purpose of the Study:
- To discover novel human lung cancer-specific peptides using in vivo phage display screening.
- To evaluate the tumor-targeting capacity of discovered peptides in preclinical models.
Main Methods:
- Utilized a xenograft mouse model mimicking the tumor microenvironment for in vivo peptide-displayed phage screening.
- Employed four rounds of biopanning on A549-derived xenograft tumors.
- Validated peptide targeting via whole-body imaging, in vitro cell-binding assays, and immunohistochemistry.
Main Results:
- Identified novel peptides that specifically accumulate in adenocarcinoma lung cancer xenograft tissues.
- Demonstrated intense binding of a selected peptide to lung cancer cells both in vitro and in vivo.
- Confirmed specificity through competition assays with unlabeled phages.
Conclusions:
- Successfully discovered peptides with specific targeting capabilities for human lung cancer.
- These peptides hold significant promise for developing novel targeted therapeutics and diagnostic imaging agents.
- The findings support the feasibility of using these peptides in advanced drug delivery systems.
