title: A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells.
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.
authors.affiliation: Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
authors.forename: Malay
authors.initials: M
authors.lastname: Patra
authors.affiliation: Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
authors.forename: Timothy C
authors.initials: TC
authors.lastname: Johnstone
authors.affiliation: Department of Chemistry, King's College London, London, SE1 1DB, UK.
authors.forename: Kogularamanan
authors.initials: K
authors.lastname: Suntharalingam
authors.affiliation: Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA. lippard@mit.edu.
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Lippard
mesh_terms: D045744:Cell Line, Tumor; D005947:Glucose / Q000737:chemistry*; D006801:Humans; D009004:Monosaccharide Transport Proteins / Q000378:metabolism*; D009369:Neoplasms / Q000378:metabolism*; D010984:Platinum / Q000737:chemistry*
chemical_list: D009004:Monosaccharide Transport Proteins; D010984:Platinum; D005947:Glucose
keywords: antitumor agents; glucose transporters; glycoconjugates; medicinal inorganic chemistry; platinum