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A Potent Glucose–Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells
Author(s) -
Patra Malay,
Johnstone Timothy C.,
Suntharalingam Kogularamanan,
Lippard Stephen J.
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201510551
Subject(s) - cytotoxicity , glucose transporter , cancer cell , chemistry , glucose uptake , platinum , in vitro , transporter , conjugate , biochemistry , cancer , cancer research , biology , gene , endocrinology , insulin , catalysis , mathematical analysis , genetics , mathematics
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.