✦ LIBER ✦

Dinuclear Alkylamine Platinum(II) Complexes of [1,2-Bis(4-fluorophenyl)ethylenediamine]platinum(II): Influence of Endocytosis and Copper and Organic Cation Transport Systems on Cellular Uptake

✍ Scribed by Timo Kapp; Stefanie Müller; Ronald Gust

Publisher: John Wiley and Sons
Year: 2006
Tongue: English
Weight: 168 KB
Volume: 1
Category: Article
ISSN: 1860-7179
DOI: 10.1002/cmdc.200500096

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✦ Synopsis

Abstract

Various possible pathways for the uptake of cationic alkylamine platinum(II) complexes into the MCF‐7 breast cancer cells were studied with di[meso‐1,2‐bis(4‐fluorophenyl)ethylenediamine]di[sulfinylbis(methane)‐S][μ‐1,6‐diaminohexaneN:N′]diplatinum(II) disulfate (m‐4F‐PtDMSO‐DAH) as an example. It was demonstrated that m‐4F‐PtDMSO‐DAH competed neither for the copper transporter nor the organic cation transporters (OCT and OATP). Instead, adsorptive endocytosis by macropinocytosis played an essential role. Inhibitors of this processes such as amiloride, N‐ethyl‐N‐isopropylamiloride (EIPA), wortmannin, and cytochalasin D decreased the intracellular uptake of m‐4F‐PtDMSO‐DAH dramatically. These results support the understanding of the pharmacological behavior of this promising drug family, which showed no cross resistance with cisplatin.

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