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

Malay Patra; Timothy C. Johnstone; Kogularamanan Suntharalingam; Stephen J. Lippard

doi:10.1002/anie.201510551

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

Malay Patra, Timothy C. Johnstone, Kogularamanan Suntharalingam, Stephen J. Lippard^*

^*Corresponding author for this work

Chemistry

Research output: Contribution to journal › Article › peer-review

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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. Glucose-platinum conjugates for targeted delivery: A rationally designed potent glucose-platinum conjugate exploits glucose transporters, which are widely overexpressed in cancers, for internalization and selectively accumulates in and annihilates cancer cells.

Original language	English
Pages (from-to)	2550-2554
Number of pages	5
Journal	ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume	55
Issue number	7
Early online date	8 Jan 2016
DOIs	https://doi.org/10.1002/anie.201510551
Publication status	Published - 12 Feb 2016

Keywords

antitumor agents
glucose transporters
glycoconjugates
medicinal inorganic chemistry
platinum

UN SDGs

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10.1002/anie.201510551

A Potent Glucose–Platinum_PATRA_Accepted9Dec2015_GREEN AAMAccepted author manuscript, 734 KB

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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. Glucose-platinum conjugates for targeted delivery: A rationally designed potent glucose-platinum conjugate exploits glucose transporters, which are widely overexpressed in cancers, for internalization and selectively accumulates in and annihilates cancer cells.",

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AU - Patra, Malay

AU - Johnstone, Timothy C.

AU - Suntharalingam, Kogularamanan

AU - Lippard, Stephen J.

PY - 2016/2/12

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KW - glucose transporters

KW - glycoconjugates

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KW - platinum

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

Abstract

Keywords

UN SDGs

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