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Publikācija: Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Jekaterīna Ivanova
Vaida Morkunaite
Lina Baranauskiene
Asta Zubriene
Visvaldas Kairys
Peteris Trapencieris
Daumantas Matulis
Atslēgas vārdi
Anotācija 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/ 
Atsauce 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
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ID 24037