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Boronate-Mediated Biologic Delivery
Author(s) -
Gregory A. Ellis,
Michael J. Palte,
Ronald T. Raines
Publication year - 2012
Publication title -
journal of the american chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 7.115
H-Index - 612
eISSN - 1520-5126
pISSN - 0002-7863
DOI - 10.1021/ja210719s
Subject(s) - chemistry , macromolecule , cytosol , boronic acid , delivery system , biochemistry , drug delivery , combinatorial chemistry , organic chemistry , enzyme , pharmacology , medicine
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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