Tailored Multivalent Neo-Glycoproteins: Synthesis, Evaluation, and Application of a Library of Galectin-3-Binding Glycan Ligands

Bioconjug Chem. 2017 Nov 15;28(11):2832-2840. doi: 10.1021/acs.bioconjchem.7b00520. Epub 2017 Oct 18.

Abstract

Galectin-3 (Gal-3), a member of the β-galactoside-binding lectin family, is a tumor biomarker and involved in tumor angiogenesis and metastasis. Gal-3 is therefore considered as a promising target for early cancer diagnosis and anticancer therapy. We here present the synthesis of a library of tailored multivalent neo-glycoproteins and evaluate their Gal-3 binding properties. By the combinatorial use of glycosyltransferases and chemo-enzymatic reactions, we first synthesized a set of N-acetyllactosamine (Galβ1,4GlcNAc; LacNAc type 2)-based oligosaccharides featuring five different terminating glycosylation epitopes, respectively. Neo-glycosylation of bovine serum albumin (BSA) was accomplished by dialkyl squarate coupling to lysine residues resulting in a library of defined multivalent neo-glycoproteins. Solid-phase binding assays with immobilized neo-glycoproteins revealed distinct affinity and specificity of the multivalent glycan epitopes for Gal-3 binding. In particular, neo-glycoproteins decorated with N',N″-diacetyllactosamine (GalNAcβ1,4GlcNAc; LacdiNAc) epitopes showed high selectivity and were demonstrated to capture Gal-3 from human serum with high affinity. Furthermore, neo-glycoproteins with terminal biotinylated LacNAc glycan motif could be utilized as Gal-3 detection agents in a sandwich enzyme-linked immunosorbent assay format. We conclude that, in contrast to antibody-based capture steps, the presented neo-glycoproteins are highly useful to detect functionally intact Gal-3 with high selectivity and avidity. We further gain novel insights into the binding affinity of Gal-3 using tailored multivalent neo-glycoproteins, which have the potential for an application in the context of cancer-related biomedical research.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Sugars / chemical synthesis
  • Amino Sugars / chemistry
  • Amino Sugars / metabolism
  • Animals
  • Cattle
  • Combinatorial Chemistry Techniques
  • Galectin 3 / antagonists & inhibitors*
  • Galectin 3 / metabolism*
  • Glycoproteins / chemical synthesis
  • Glycoproteins / chemistry*
  • Glycoproteins / metabolism
  • Glycoproteins / pharmacology*
  • Glycosylation
  • Humans
  • Ligands
  • Oligosaccharides / chemical synthesis
  • Oligosaccharides / chemistry
  • Oligosaccharides / metabolism
  • Protein Binding
  • Serum Albumin, Bovine / chemical synthesis
  • Serum Albumin, Bovine / chemistry
  • Serum Albumin, Bovine / metabolism
  • Serum Albumin, Bovine / pharmacology

Substances

  • Amino Sugars
  • Galectin 3
  • Glycoproteins
  • Ligands
  • Oligosaccharides
  • Serum Albumin, Bovine
  • N-acetyllactosamine