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Synthesis and biological evaluation of tumor targetedlysosomotropic detergents

Wolf, Markus

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Abstract

Conjugation of a lysosomotropic detergent to tumor affine peptides (octreotate and melanocortin analogous) resulted in receptor mediated uptake of the peptide conjugates into tumor cells expressing the peptide receptors. During intracellular trafficking the lysosomotropic detergent was cleaved from the peptide. Cytotoxicity studies showed IC50 values in the range of 11-72 µM caused by lysosomal rupture as proven by confocal laser scanning microscopy. For cells not expressing the receptors the conjugates were less cytotoxic.

Item Type: Other
Date Deposited: 23 Jul 2007 12:16
Date: 2007
Faculties / Institutes: Service facilities > German Cancer Research Center (DKFZ)
Subjects: 570 Life sciences
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