A Platinum(IV) Prodrug-Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain.
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ABSTRACT:
SUBMITTER: Fadzen CM
PROVIDER: S-EPMC7992430 | biostudies-literature | 2020 Jul
REPOSITORIES: biostudies-literature
Publications
A Platinum(IV) Prodrug-Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain.
Fadzen Colin M CM Wolfe Justin M JM Zhou Wen W Cho Choi-Fong CF von Spreckelsen Niklas N Hutchinson Kathryn T KT Lee Yen-Chun YC Chiocca E Antonio EA Lawler Sean E SE Yilmaz Omer H OH Lippard Stephen J SJ Pentelute Bradley L BL
Journal of medicinal chemistry 20200626 13
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 af ...[more]
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