Journal
FUTURE MEDICINAL CHEMISTRY
Volume 10, Issue 6, Pages 619-629Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0183
Keywords
antitumor agent; pharmacokinetics; triple-helical peptide
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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. [GRAPHICS] .
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