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Mathematisch-Naturwissenschaftliche Fakultät - Jahrgang 2010


Titel Cellular Influx and Cytotoxicity of Oxaliplatin Analogues
Autor Irina Buß
Publikationsform Dissertation
Abstract This thesis describes the first systematic investigation of the relationship between lipophilicity and reactivity on the one hand and cellular accumulation and cytotoxic activity on the other hand of a new class of oxaliplatin derivatives with different substituents at position 4 of the cyclohexane ring and different leaving ligands. Furthermore, the contribution of hCTR1 and hOCT1-3 on the influx of oxaliplatin was investigated. Information regarding the influence of oxaliplatin on the expression of these transporters, as well as on their localization inside cancer cells is still limited. In contrast to the studies conducted in the past, in this study no transfected cell lines were used.
Lipophilicity and reactivity are important determinants of the platinum influx. In contrast to the early influx phase, in which lipophilicity predominantly governs the influx rate, the late influx phase is mainly controlled by the reactivity of a platinum compound. Passive diffusion is suggested as the preponderant influx mechanism in the early influx phase and protein-mediated transport as the major influx mechanism in the late influx phase. more...
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© Universitäts- und Landesbibliothek Bonn | Veröffentlicht: 08.10.2010