Boronate-Mediated Biologic Delivery

Gregory A. Ellis, Michael J. Palte, and Ronald T. Raines*§
Department of Biochemistry, Medical Scientist Training Program and Molecular & Cellular Pharmacology Graduate Training Program, and §Department of Chemistry, University of Wisconsin-Madison, Madison, Wisconsin 53706, United States
J. Am. Chem. Soc.2012134 (8), pp 3631–3634
DOI: 10.1021/ja210719s
Publication Date (Web): February 3, 2012
Copyright © 2012 American Chemical Society




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.

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