Issue 13, 2012
From the journal:

Chemical Communications

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

Fabrizio Carta,a   Mayank Aggarwal,b   Alfonso Maresca,a   Andrea Scozzafava,a   Robert McKenna*b  and  Claudiu T. Supuran*a  

* Corresponding authors

a Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
E-mail: claudiu.supuran@unifi.it

b Department of Biochemistry and Molecular Biology, College of Medicine, University of Florida, Box 100245, Gainesville, USA
E-mail: rmckenna@ufl.edu
Fax: +1 352 392-3422
Tel: +1 352 392-5696

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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Article information

DOI
https://doi.org/10.1039/C2CC16395K
Article type
Communication
Submitted
14 Oct 2011
Accepted
12 Dec 2011
First published
14 Dec 2011

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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