| Literature DB >> 32410451 |
Colin M Fadzen1, Justin M Wolfe1, Wen Zhou1,2, Choi-Fong Cho3, Niklas von Spreckelsen3,4, Kathryn T Hutchinson3, Yen-Chun Lee1, E Antonio Chiocca3, Sean E Lawler3, Omer H Yilmaz2, Stephen J Lippard1, Bradley L Pentelute1,2.
Abstract
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.Entities:
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Year: 2020 PMID： 32410451 DOI： 10.1021/acs.jmedchem.0c00022
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446