Development of a carboplatin derivative conjugated with a collagen-like triple-helical peptide. (7th February 2018)

• Record Type: Journal Article
• Authors: Masuda, Ryo; Hayashi, Risa; Nose, Hiroshi; Taguchi, Akihiro; Hayashi, Yoshio; Yasui, Hiroyuki; Koide, Takaki
• Is Part Of: Future medicinal chemistry. Volume 10:Number 6(2018)
• Page Start: 619
• Page End: 629
• Publication Date: 2018-02-07
• Subjects: antitumor agent -- pharmacokinetics -- triple-helical peptide; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc-2017-0183
• Languages: English
• ISSNs: 1756-8919

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. Graphical abstract: