A Strategy for Tumor Targeting by Higher‐Order Glycan Pattern Recognition: Synthesis and In Vitro and In Vivo Properties of Glycoalbumins Conjugated with Four Different N‐Glycan Molecules

Natural glycoconjugates that form glycocalyx play important roles in various biological processes based on cell surface recognition through pattern recognition mechanisms. This work represents a new synthesis‐based screening strategy to efficiently target the cancer cells by higher‐order glycan patt...

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Published in:Small (Weinheim an der Bergstrasse, Germany) Germany), 2020-11, Vol.16 (46), p.e2004831-n/a
Main Authors: Smirnov, Ivan, Sibgatullina, Regina, Urano, Sayaka, Tahara, Tsuyoshi, Ahmadi, Peni, Watanabe, Yasuyoshi, Pradipta, Ambara R., Kurbangalieva, Almira, Tanaka, Katsunori
Format: Article
Language:English
Subjects:
biodistribution
Biological activity
Cancer
Chemical compounds
Chemical reactions
Diagnostic systems
Glycan
higher‐order heterogeneity
Imines
Nanotechnology
N‐glycoalbumins
Pattern recognition
Pharmacology
Strategy
tumor targeting
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Summary:Natural glycoconjugates that form glycocalyx play important roles in various biological processes based on cell surface recognition through pattern recognition mechanisms. This work represents a new synthesis‐based screening strategy to efficiently target the cancer cells by higher‐order glycan pattern recognition in both cells and intact animals (mice). The use of the very fast, selective, and effective RIKEN click reaction (6π‐azaelectrocyclization of unsaturated imines) allows to synthesize and screen various structurally well‐defined glycoalbumins containing two and eventually four different N‐glycan structures in a very short time. The importance of glycan pattern recognition is exemplified in both cell‐ and mouse‐based experiments. The use of pattern recognition mechanisms for cell targeting represents a novel and promising strategy for the development of diagnostic, prophylactic, and therapeutic agents for various diseases including cancers. Very fast and selective RIKEN click reaction allows to synthesize and screen various structurally well‐defined glycoalbumins containing four different N‐glycan structures in a very short time. Pattern recognition mechanisms for cell targeting in mice represent a novel and promising strategy for diagnostic, prophylactic, and therapeutic agents for various diseases, including cancers.
ISSN:1613-6810
1613-6829
DOI:10.1002/smll.202004831