Molecularly Imprinted Microgels as Enzyme Inhibitors

被引:244
作者
Cutivet, Arnaud [1 ]
Schembri, Carol [1 ]
Kovensky, Jose [2 ]
Haupt, Karsten [1 ]
机构
[1] Univ Technol Compiegne, Dept Bioengn, CNRS, UMR 6022, F-60205 Compiegne, France
[2] Jules Verne Univ Picardy, Carbohydrate Lab, CNRS, UMR 6219, F-80039 Amiens, France
关键词
POLYMERS; PROTEINS; NANOGELS; BINDING; TRYPSIN; MIMICS;
D O I
10.1021/ja901600e
中图分类号
O6 [化学];
学科分类号
070301 [无机化学];
摘要
We demonstrate, on the example of trypsin, the use of water-soluble molecularly imprinted polymer microgels as specific enzyme inhibitors. Using a strong anchoring monomer, methacryloylaminobenzamidne, the growing polymer chains are confined to close proximity of the substrate recognition site of our model enzyme. The microgels bind selectively trypsin over other proteins of similar size and molecular weight, and show competitive inhibition of trypsin with an inhibition constant K-i of 79 nM, making them more potent inhibitors than the low molecular-weight competitive inhibitor benzamidine by almost 3 orders of magnitude. We believe that these tailor-made materials with biological activity have potential for future drug development that extends beyond enzyme inhibition.
引用
收藏
页码:14699 / 14702
页数:4
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