A Platinum(IV) Prodrug - Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain

Colin M. Fadzen, Justin M. Wolfe, Wen Zhou, Choi Fong Cho, Niklas Von Spreckelsen, Kathryn T. Hutchinson, Yen Chun Lee, E. Antonio Chiocca, Sean E. Lawler, Omer H. Yilmaz, Stephen J. Lippard, Bradley L. Pentelute

研究成果: Article同行評審

21 引文 斯高帕斯(Scopus)

摘要

Effective delivery to the brain limits the development of novel glioblastoma therapies. Here, we introduce conjugation between platinum(IV) prodrugs of cisplatin and perfluoroaryl peptide macrocycles to increase brain uptake. We demonstrate that one such conjugate shows efficacy against glioma stem-like cells. We investigate the pharmacokinetics of this conjugate in mice and show that the amount of platinum in the brain after treatment with the conjugate is 15-fold greater than with cisplatin after 5 h.

原文English
頁(從 - 到)6741-6747
頁數7
期刊Journal of Medicinal Chemistry
63
發行號13
DOIs
出版狀態Published - 2020 7月 9

All Science Journal Classification (ASJC) codes

  • 分子醫學
  • 藥物發現

指紋

深入研究「A Platinum(IV) Prodrug - Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain」主題。共同形成了獨特的指紋。

引用此