Boronate-Mediated Biologic Delivery

被引:199
作者
Ellis, Gregory A. [1 ]
Palte, Michael J. [2 ,3 ]
Raines, Ronald T. [1 ,4 ]
机构
[1] Univ Wisconsin, Dept Biochem, Madison, WI 53706 USA
[2] Univ Wisconsin, Med Scientist Training Program, Madison, WI 53706 USA
[3] Univ Wisconsin, Mol & Cellular Pharmacol Grad Training Program, Madison, WI 53706 USA
[4] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA
关键词
DRUG-DELIVERY; RIBONUCLEASE INHIBITOR; PHENYLBORONIC ACID; CELL-MEMBRANE; EFFICIENT; RECEPTOR; PROTEIN; CANCER; THERAPEUTICS; THERAPY;
D O I
10.1021/ja210719s
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:3631 / 3634
页数:4
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