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dc.contributor.authorFadzen, Colin M
dc.contributor.authorWolfe, Justin M
dc.contributor.authorZhou, Wen
dc.contributor.authorCho, Choi-Fong
dc.contributor.authorvon Spreckelsen, Niklas
dc.contributor.authorHutchinson, Kathryn T
dc.contributor.authorLee, Yen-Chun
dc.contributor.authorChiocca, E Antonio
dc.contributor.authorLawler, Sean E
dc.contributor.authorYilmaz, Omer H
dc.contributor.authorLippard, Stephen J
dc.contributor.authorPentelute, Bradley L
dc.date.accessioned2021-10-27T20:23:21Z
dc.date.available2021-10-27T20:23:21Z
dc.date.issued2020
dc.identifier.urihttps://hdl.handle.net/1721.1/135410
dc.description.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.
dc.language.isoen
dc.publisherAmerican Chemical Society (ACS)
dc.relation.isversionof10.1021/ACS.JMEDCHEM.0C00022
dc.rightsCreative Commons Attribution-Noncommercial-Share Alike
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/
dc.sourcePMC
dc.titleA Platinum(IV) Prodrug—Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain
dc.typeArticle
dc.contributor.departmentMassachusetts Institute of Technology. Department of Chemistry
dc.contributor.departmentKoch Institute for Integrative Cancer Research at MIT
dc.relation.journalJournal of Medicinal Chemistry
dc.eprint.versionAuthor's final manuscript
dc.type.urihttp://purl.org/eprint/type/JournalArticle
eprint.statushttp://purl.org/eprint/status/PeerReviewed
dc.date.updated2021-04-27T18:34:39Z
dspace.orderedauthorsFadzen, CM; Wolfe, JM; Zhou, W; Cho, C-F; von Spreckelsen, N; Hutchinson, KT; Lee, Y-C; Chiocca, EA; Lawler, SE; Yilmaz, OH; Lippard, SJ; Pentelute, BL
dspace.date.submission2021-04-27T18:34:42Z
mit.journal.volume63
mit.journal.issue13
mit.licenseOPEN_ACCESS_POLICY
mit.metadata.statusAuthority Work and Publication Information Needed


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