Abstract
Aim: The development of a platinum anticancer agent that has improved efficacy by efficient delivery to a tumor and that suppresses side effects has been investigated. Arginine-rich triple-helical peptides are promising drug carriers because of their stability in body fluids and cell-penetrating activity. Results: We synthesized a carboplatin derivative conjugated with an arginine-rich triple-helical peptide. This derivative released platinum under acidic conditions or in the presence Cl- ions. Administration of this derivative to P388 tumor-bearing mice showed comparable survival rates to twice the dose of carboplatin, which was attributed to a longer mean residence time by pharmacokinetics analysis. Conclusion: The collagen-like triple-helical peptide was an efficient carrier of a platinum anticancer agent because of a modification to its pharmacokinetic profile.
Original language | English |
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Pages (from-to) | 619-629 |
Number of pages | 11 |
Journal | Future Medicinal Chemistry |
Volume | 10 |
Issue number | 6 |
DOIs | |
Publication status | Published - 2018 Mar |
Keywords
- antitumor agent
- pharmacokinetics
- triple-helical peptide
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery