Development of a carboplatin derivative conjugated with a collagen-like triple-helical peptide

Ryo Masuda, Risa Hayashi, Hiroshi Nose, Akihiro Taguchi, Yoshio Hayashi, Hiroyuki Yasui, Takaki Koide*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

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 languageEnglish
Pages (from-to)619-629
Number of pages11
JournalFuture Medicinal Chemistry
Volume10
Issue number6
DOIs
Publication statusPublished - 2018 Mar

Keywords

  • antitumor agent
  • pharmacokinetics
  • triple-helical peptide

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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