Fadzen, Colin M., Wolfe, Justin M., Zhou, Wen, Cho, Choi-Fong, von Spreckelsen, Niklas ORCID: 0000-0002-9873-1711, Hutchinson, Kathryn T., Lee, Yen-Chun, Chiocca, E. Antonio, Lawler, Sean E., Yilmaz, Omer H., Lippard, Stephen J. and Pentelute, Bradley L. (2020). A Platinum(IV) Prodrug-Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain. J. Med. Chem., 63 (13). S. 6741 - 6748. WASHINGTON: AMER CHEMICAL SOC. ISSN 1520-4804

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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.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Fadzen, Colin M.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Wolfe, Justin M.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Zhou, WenUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Cho, Choi-FongUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
von Spreckelsen, NiklasUNSPECIFIEDorcid.org/0000-0002-9873-1711UNSPECIFIED
Hutchinson, Kathryn T.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Lee, Yen-ChunUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Chiocca, E. AntonioUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Lawler, Sean E.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Yilmaz, Omer H.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Lippard, Stephen J.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Pentelute, Bradley L.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
URN: urn:nbn:de:hbz:38-326645
DOI: 10.1021/acs.jmedchem.0c00022
Journal or Publication Title: J. Med. Chem.
Volume: 63
Number: 13
Page Range: S. 6741 - 6748
Date: 2020
Publisher: AMER CHEMICAL SOC
Place of Publication: WASHINGTON
ISSN: 1520-4804
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
TRANSITION-METAL-COMPLEXES; DRUG DESIGN; PHASE-II; IN-VITRO; CISPLATIN; CARBOPLATIN; GLIOMA; TUMOR; PHARMACOKINETICS; CELLSMultiple languages
Chemistry, MedicinalMultiple languages
URI: http://kups.ub.uni-koeln.de/id/eprint/32664

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