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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 γ-carbonic anhydrase from the oral pathogen Porphyromonas gingivalis
Bioorganic and Medicinal Chemistry Letters, Volume 24, No. 1, Year 2014
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Description
A carbonic anhydrase (CA, EC 4.2.1.1) denominated PgiCA, belonging to the γ-class, from the oral pathogenic bacteria Porphyromonas gingivalis, the main causative agent of periodontitis, was investigated for its inhibition profile with sulfonamides and one sulfamate. Dichlorophenamide, topiramate and many simple aromatic/heterocyclic sulfonamides were ineffective as PgiCA inhibitors whereas the best inhibition was observed with halogenosulfanilamides incorporating heavy halogens, 4-hydroxy-and 4-hydroxyalkyl-benzenesulfonamides, acetazolamide, methazolamide, zonisamide, indisulam, celecoxib, saccharin and hydrochlorothiazide (KIs in the range of 131-380 nM). The inhibition profile of PgiCA was very different from that of CAM, hCA I and II or the β-CA from a protozoan parasite (Leishmania donovani chagasii). Identification of potent and possibly selective inhibitors of PgiCA may lead to pharmacological tools useful for understanding the physiological role(s) of this enzyme. © 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: 52
Authors: 8
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2013.11.030
ISSN:
0960894X
e-ISSN:
14643405
Research Areas
Health System And Policy