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

Author(s)
Fadzen, Colin M; Wolfe, Justin M; Zhou, Wen; Cho, Choi-Fong; von Spreckelsen, Niklas; ... Show more
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Abstract
© 2020 American Chemical Society. 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.
Date issued
2020
URI
https://hdl.handle.net/1721.1/135410
Department
Massachusetts Institute of Technology. Department of Chemistry; Koch Institute for Integrative Cancer Research at MIT
Journal
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
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