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Piperidine-based glycodendrons as protein N-glycan prosthetics

Bioorganic & Medicinal Chemistry, ISSN: 0968-0896, Vol: 24, Issue: 20, Page: 4791-4800
2016
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Article Description

The generation of homogeneously glycosylated proteins is essential for defining glycoform-specific activity and improving protein-based therapeutics. We present a novel glycodendron prosthetic which can be site-selectively appended to recombinant proteins to create ‘ N -glycosylated’ glycoprotein mimics. Using computational modeling, we designed the dendrimer scaffold and protein attachment point to resemble the native N-glycan architecture. Three piperidine–melamine glycodendrimers were synthesized via a chemoenzymatic route and attached to human growth hormone and the F c region of human IgG. These products represent a new class of engineered biosimilars bearing novel glycodendrimer structures.

Bibliographic Details

Hudak, Jason E; Belardi, Brian; Appel, Mason J; Solania, Angelo; Robinson, Peter V; Bertozzi, Carolyn R

Elsevier BV

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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