A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells
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Author(s)
Suntharalingam, Kogularamanan
Patra, Malay
Johnstone, Timothy
Lippard, Stephen J.
Date Issued
February 2016
Journal
Angewandte Chemie International Edition
Publisher
Wiley Blackwell
Citation
Patra, Malay; Johnstone, Timothy C.; Suntharalingam, Kogularamanan and Lippard, Stephen J. “A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells.” Angewandte Chemie International Edition 55, no. 7 (January 2016): 2550–2554 © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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Author's final manuscript
Abstract
Three rationally designed glucose–platinum conjugates (Glc–Pts) were synthesized and their biological activities evaluated. The Glc–Pts, 1–3, exhibit high levels of cytotoxicity toward a panel of cancer cells. The subcellular target and cellular uptake mechanism of the Glc–Pts were elucidated. For uptake into cells, Glc–Pt 1 exploits both glucose and organic cation transporters, both widely overexpressed in cancer. Compound 1 preferentially accumulates in and annihilates cancer, compared to normal epithelial, cells in vitro.
MIT Department
Massachusetts Institute of Technology. Department of Chemistry
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DOI of Published Version
https://doi.org/10.1002/anie.201510551
