Dimerization of a cell-penetrating peptide leads to enhanced cellular uptake and drug delivery

• Jan Hoyer,
• Ulrich Schatzschneider,
• Michaela Schulz-Siegmund and
• Ines Neundorf

Beilstein J. Org. Chem. 2012, 8, 1788–1797, doi:10.3762/bjoc.8.204

• (cymantrene) complexes to tumor cell lines, inducing high cellular toxicity. In order to increase the potential of the organometallic complexes to kill tumor cells, we were looking for a way to enhance cellular uptake. Therefore, we designed a branched dimeric variant of sC18, (sC18)2, which was shown to have

• potential due to limited bioavailability and cellular uptake. In recent years, cell-penetrating peptides (CPPs) emerged as an encouraging tool to overcome this obstacle owing to their ability to autonomously cross the cellular membrane in a receptor-independent manner. This enables them to deliver a large

• the peptides, which is considered to be crucial for initial membrane interaction through binding to negatively charged phospholipids and glycosaminoglycans [6]. Endocytic and non-endocytic processes have been proposed to be involved in cellular uptake; however, the exact mechanism triggering

Unprecedented deoxygenation at C-7 of the ansamitocin core during mutasynthetic biotransformations

• Tobias Knobloch,
• Gerald Dräger,
• Wera Collisi,
• Florenz Sasse and
• Andreas Kirschning

Beilstein J. Org. Chem. 2012, 8, 861–869, doi:10.3762/bjoc.8.96

• ]. Producer strains genetically blocked in the biosynthesis of important and complex natural products can serve as such new tools. The synthetic concept based on these blocked mutants is termed “mutational biosynthesis”, or in short mutasynthesis, and it relies on the cellular uptake of modified biosynthetic

An easily accessible sulfated saccharide mimetic inhibits in vitro human tumor cell adhesion and angiogenesis of vascular endothelial cells

• Grazia Marano,
• Claas Gronewold,
• Martin Frank,
• Anette Merling,
• Christian Kliem,
• Sandra Sauer,
• Manfred Wiessler,
• Eva Frei and
• Reinhard Schwartz-Albiez

Beilstein J. Org. Chem. 2012, 8, 787–803, doi:10.3762/bjoc.8.89

• gelatinase MMP-2 and its proforms could also be caused by lower pro-MMP-2 expression upon GSF binding or its cellular uptake. Effects of saccharide mimetics on adhesion, migration and tubule formation of vascular endothelial cells Endothelial cells play a central role in the process of angiogenesis, which is