A Potent Glucose–Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells. (8th January 2016)

• Record Type: Journal Article
• Authors: Patra, Malay; Johnstone, Timothy C.; Suntharalingam, Kogularamanan; Lippard, Stephen J.
• Is Part Of: Angewandte Chemie. Volume 128:Number 7(2016)
• Page Start: 2596
• Page End: 2600
• Publication Date: 2016-01-08
• Subjects: Glucosetransporter -- Glykokonjugate -- Medizinische anorganische Chemie -- Platin -- Tumortherapeutika; Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201510551
• Languages: English
• ISSNs: 0044-8249

Abstract

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–Pt1 exploits both glucose and organic cation transporters, both widely overexpressed in cancer. Compound1 preferentially accumulates in and annihilates cancer, compared to normal epithelial, cells in vitro.