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Fluorescent Silica Nanoparticles with Multivalent Inhibitory Effects towards Carbonic Anhydrases
Author(s) -
Touisni Nadia,
Kanfar Nasreddine,
Ulrich Sébastien,
Dumy Pascal,
Supuran Claudiu T.,
Mehdi Ahmad,
Winum JeanYves
Publication year - 2015
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201501037
Subject(s) - carbonic anhydrase , chemistry , enzyme , cytosol , fluorescence , isozyme , biochemistry , nanoparticle , gene isoform , sulfonamide , transmembrane protein , inhibitory postsynaptic potential , combinatorial chemistry , biophysics , stereochemistry , receptor , nanotechnology , biology , physics , materials science , quantum mechanics , neuroscience , gene
Multifunctional silica nanoparticles decorated with fluorescent and sulfonamide carbonic anhydrase (CA) inhibitors were prepared and investigated as multivalent enzyme inhibitors against the cytosolic isoforms hCA I and II and the transmembrane tumor‐associated ones hCA IX and XII. Excellent inhibitory effects were observed with these nanoparticles, with K I values in the low nanomolar range (6.2–0.67 n M ) against all tested isozymes. A significant multivalency effect was seen for the inhibition of the monomeric enzymes hCA I and II compared to the dimeric hCA IX and hCA XII isoforms, where no multivalent effect was observed, suggesting that the multivalent binding is occurring through enzyme clustering.