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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Sulfonamide inhibition studies of the δ-carbonic anhydrase from the diatom Thalassiosira weissflogii
Bioorganic and Medicinal Chemistry Letters, Volume 24, No. 1, Year 2014
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Description
The δ-carbonic anhydrase (CA, EC 4.2.1.1) TweCA from the marine diatom Thalassiosira weissflogii has recently been cloned, purified and its activity/inhibition with anions investigated. Here we report the first sulfonamide/sulfamate inhibition study of a δ-class CA. Among the 40 such compounds investigated so far, 3-bromosulfanilamide, acetazolamide, ethoxzolamide, dorzolamide and brinzolamide were the most effective TweCA inhibitors detected, with KIs of 49.6-118 nM. Many simple aromatic sulfonamides as well as dichlorophenamide, benzolamide, topiramate, zonisamide, indisulam and valdecoxib were medium potency inhibitors, (KIs of 375-897 nM). Saccharin and hydrochlorothiazide were ineffective inhibitors of the δ-class enzyme, with KIs of 4.27-9.20 μM. The inhibition profile of the δ-CA is very different from that of α-, β-and γ-CAs from different organisms. Although no X-ray crystal structure of this enzyme is available, we hypothesize that as for other CA classes, the sulfonamides inhibit the enzymatic activity by binding to the Zn(II) ion from the δ-CA active site. © 2013 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Vullo, Daniela
Italy, Florence
Università Degli Studi Di Firenze
del Prete, Sonia
Italy, Naples
Istituto Di Biochimica Delle Proteine, Naples
Osman, Sameh M.
Saudi Arabia, Riyadh
College of Sciences
De Luca, Viviana
Italy, Naples
Istituto Di Biochimica Delle Proteine, Naples
Scozzafava, A.
Italy, Florence
Università Degli Studi Di Firenze
ALOthman, Zeid A.
Saudi Arabia, Riyadh
College of Sciences
Supuran, Claudiu T.
Italy, Florence
Università Degli Studi Di Firenze
Saudi Arabia, Riyadh
College of Sciences
Capasso, Clemente
Italy, Naples
Istituto Di Biochimica Delle Proteine, Naples
Statistics
Citations: 54
Authors: 8
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2013.11.021
ISSN:
0960894X
e-ISSN:
14643405