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Biomedicines 2017, 5(2), 14; doi:10.3390/biomedicines5020014

Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies

1
Institut für Laboratoriumsmedizin, Klinische Chemie und Pathobiochemie, Charité—Universitätsmedizin Berlin, Campus Virchow-Klinikum, 13353 Berlin, Germany
2
Institut für Pharmazie, Freie Universität Berlin, 14195 Berlin, Germany
3
Institut für Lebensmittelchemie, TU Braunschweig, 38106 Braunschweig, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Stefan Barth
Received: 10 February 2017 / Revised: 21 March 2017 / Accepted: 24 March 2017 / Published: 29 March 2017
(This article belongs to the Special Issue Targeted Human Cytolytic Fusion Proteins)
View Full-Text   |   Download PDF [2524 KB, uploaded 29 March 2017]   |  

Abstract

Protein-based targeted toxins play an increasingly important role in targeted tumor therapies. In spite of their high intrinsic toxicity, their efficacy in animal models is low. A major reason for this is the limited entry of the toxin into the cytosol of the target cell, which is required to mediate the fatal effect. Target receptor bound and internalized toxins are mostly either recycled back to the cell surface or lysosomally degraded. This might explain why no antibody-targeted protein toxin has been approved for tumor therapeutic applications by the authorities to date although more than 500 targeted toxins have been developed within the last decades. To overcome the problem of insufficient endosomal escape, a number of strategies that make use of diverse chemicals, cell-penetrating or fusogenic peptides, and light-induced techniques were designed to weaken the membrane integrity of endosomes. This review focuses on glycosylated triterpenoids as endosomal escape enhancers and throws light on their structure, the mechanism of action, and on their efficacy in cell culture and animal models. Obstacles, challenges, opportunities, and future prospects are discussed. View Full-Text
Keywords: saponins; endosomal escape; efficacy enhancers; targeted toxins; immunotoxins; cytosolic drug delivery; controlled drug release; cancer treatment; endocytosis saponins; endosomal escape; efficacy enhancers; targeted toxins; immunotoxins; cytosolic drug delivery; controlled drug release; cancer treatment; endocytosis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Fuchs, H.; Niesler, N.; Trautner, A.; Sama, S.; Jerz, G.; Panjideh, H.; Weng, A. Glycosylated Triterpenoids as Endosomal Escape Enhancers in Targeted Tumor Therapies. Biomedicines 2017, 5, 14.

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