Schneider, Hendrik; Englert, Simon; Palacios, Arturo Macarron; Romero, Jorge Alberto Lerma; Ali, Ataurehman; Avrutina, Olga; Kolmar, Harald published an article in 2021. The article was titled 《Synthetic integrin-targeting dextran-Fc hybrids efficiently inhibit tumor proliferation in vitro》, and you may find the article in Frontiers in Chemistry (Lausanne, Switzerland).Related Products of 51644-96-3 The information in the text is summarized as follows:
Herein, we present the design, synthesis, and biol. evaluation of novel integrin-targeting mol. hybrids combining RGD peptides and a potent cytotoxin presented on dextran polysaccharides. Based on an aglycosylated Fc as a centerpiece, endosomal-cleavable cytotoxic agent monomethyl auristatin E (MMAE) and dextran as multimerization site were covalently connected by two bioorthogonal enzyme-mediated reactions site-specifically. Decoration of dextran with cyclic RGD peptides, introduced by copper “”click”” reaction, resulted in the final constructs with the potential to kill integrin-overexpressing tumor cells. We found that these modifications had little impact on the stability of the Fc scaffold and the RGD-bearing construct showed good binding properties of αvβ3- expressing U87MG cells. Furthermore, the construct showed a remarkable antiproliferative activity. These results demonstrate the general capability of our design to provoke receptor-mediated endocytosis upon binding to the cellular surface, followed by endosomal cleavage of the linkage between Fc-dextran and MMAE and its subsequent release. Our approach opens new avenues to transcribe small mol. binders into tailor-made multimeric mol. hybrids with antitumor potential.tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3) was used in this study.
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3
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