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Article Dans Une Revue Journal of the American Chemical Society Année : 2009

Molecularly imprinted microgels as enzyme inhibitors

Carol Schembri
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  • PersonId : 1154897
Jose Kovensky
Karsten Haupt
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  • PersonId : 834899

Résumé

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, methacryloylaminobenzamidine, 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 Ki 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.
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Dates et versions

hal-00429186 , version 1 (01-11-2009)

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Arnaud Cutivet, Carol Schembri, Jose Kovensky, Karsten Haupt. Molecularly imprinted microgels as enzyme inhibitors. Journal of the American Chemical Society, 2009, 131 (41), pp.14699-14702. ⟨10.1021/ja901600e⟩. ⟨hal-00429186⟩
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