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Merck
CN

Molecularly imprinted microgels as enzyme inhibitors.

Journal of the American Chemical Society (2009-09-25)
Arnaud Cutivet, Carol Schembri, Jose Kovensky, Karsten Haupt
ABSTRACT

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 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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Benzamidine hydrochloride, 99%
Sigma-Aldrich
Benzamidine, ≥95.0%
Sigma-Aldrich
Benzamidine hydrochloride 1 M solution