Boronic Acid Ligands Can Target Multiple Subpopulations of Pancreatic Cancer Stem Cells via pH-Dependent Glycan-Terminal Sialic Acid Recognition

ACS Appl Bio Mater. 2021 Sep 20;4(9):6647-6651. doi: 10.1021/acsabm.1c00383. Epub 2021 May 7.

Abstract

Eradication of cancer stem cells (CSCs) is an ultimate goal in cancer chemotherapy. Although a ligand-assisted targeting approach seems rational, the existence of subpopulations of CSCs and their discrimination from those present on healthy sites makes it a severe challenge. Some boronic acid (BA) derivatives are known for the ability to bind with glycan-terminal sialic acid (SA), in a manner dependent on the acidification found in hypoxic tumoral microenvironment. Taking advantage of this feature, here we show that the BA-ligand fluorescence conjugate can effectively target multiple CSC subpopulations in parallel, which otherwise must be independently aimed when using antibody--ligands.

Keywords: active targeting; boronic acids; cancer stem cells; pancreatic cancer; sialic acids; stimuli-response.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boronic Acids / pharmacology
  • Humans
  • Hydrogen-Ion Concentration
  • Ligands
  • N-Acetylneuraminic Acid*
  • Neoplastic Stem Cells
  • Pancreatic Neoplasms* / drug therapy
  • Polysaccharides
  • Tumor Microenvironment

Substances

  • Boronic Acids
  • Ligands
  • Polysaccharides
  • N-Acetylneuraminic Acid