Boronate-mediated biologic delivery

J Am Chem Soc. 2012 Feb 29;134(8):3631-4. doi: 10.1021/ja210719s. Epub 2012 Feb 13.


Inefficient cellular delivery limits the landscape of macromolecular drugs. Boronic acids readily form boronate esters with the 1,2- and 1,3-diols of saccharides, such as those that coat the surface of mammalian cells. Here pendant boronic acids are shown to enhance the cytosolic delivery of a protein toxin. Thus, boronates are a noncationic carrier that can deliver a polar macromolecule into mammalian cells.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Boronic Acids / chemistry*
  • Boronic Acids / metabolism
  • CHO Cells
  • Cattle
  • Cell Proliferation / drug effects
  • Cricetinae
  • Cricetulus
  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Humans
  • K562 Cells
  • Models, Molecular
  • Molecular Structure
  • Ribonuclease, Pancreatic / metabolism*


  • Boronic Acids
  • Drug Carriers
  • Ribonuclease, Pancreatic