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  3. A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells

A Potent Glucose-Platinum Conjugate Exploits Glucose Transporters and Preferentially Accumulates in Cancer Cells

  • Angew Chem Int Ed Engl. 2016 Feb 12;55(7):2550-4. doi: 10.1002/anie.201510551.
Malay Patra 1,  Timothy C Johnstone 1,  Kogularamanan Suntharalingam 2,  Stephen J Lippard 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
  • 2 Department of Chemistry, King's College London, London, SE1 1DB, UK.
  • 3 Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA. lippard@mit.edu.
PMID: 26749149 DOI: 10.1002/anie.201510551
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.

Keywords

antitumor agents; glucose transporters; glycoconjugates; medicinal inorganic chemistry; platinum.

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