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Issue 13, 2012
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Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations

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Abstract

The zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1) is inhibited by several classes of zinc-binders (sulfonamides, sulfamates, and sulfamides) as well as by compounds which do not interact with the metal ion (phenols, polyamines and coumarins). Here we report a new class of potent CA inhibitors which bind the zinc ion: the dithiocarbamates (DTCs). They coordinate to the zinc ion from the enzyme active site in monodentate manner and establish many favorable interactions with amino acid residues nearby. Several low nanomolar CA I, II and IX inhibitors were detected.

Graphical abstract: Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations

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Publication details

The article was received on 14 Oct 2011, accepted on 12 Dec 2011 and first published on 14 Dec 2011


Article type: Communication
DOI: 10.1039/C2CC16395K
Chem. Commun., 2012,48, 1868-1870

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    Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations

    F. Carta, M. Aggarwal, A. Maresca, A. Scozzafava, R. McKenna and C. T. Supuran, Chem. Commun., 2012, 48, 1868
    DOI: 10.1039/C2CC16395K

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