Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII
BioMed Research International 2014
Jekaterīna Ivanova, Vaida Morkunaite, Lina Baranauskiene, Asta Zubriene, Visvaldas Kairys, Peteris Trapencieris, Daumantas Matulis

A series of modified saccharin sulfonamides have been designed as carbonic anhydrase (CA) inhibitors and synthesized. Their binding to CA isoforms I, II, VII, XII, and XIII was measured by the fluorescent thermal shift assay (FTSA) and isothermal titration calorimetry (ITC). Saccharin bound the CAs weakly, exhibiting the affinities of 1-10 mM for four CAs except CA I where binding could not be detected. Several sulfonamide-bearing saccharines exhibited strong affinities of 1-10 nM towards particular CA isoforms. The functional group binding Gibbs free energy additivity maps are presented which may provide insights into the design of compounds with increased affinity towards selected CAs.


DOI
10.1155/2014/638902
Hipersaite
https://www.hindawi.com/journals/bmri/2014/638902/

Ivanova, J., Morkunaite, V., Baranauskiene, L., Zubriene, A., Kairys, V., Trapencieris, P., Matulis, D. Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII. BioMed Research International, 2014, Vol.2014, 1.-9.lpp. ISSN 2314-6133. Pieejams: doi:10.1155/2014/638902

Publikācijas valoda
English (en)
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