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Publikācija: Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I

Publication Type Scientific article indexed in SCOPUS or WOS database
Funding for basic activity Unknown
Defending: ,
Publication language English (en)
Title in original language Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII
Field of research 1. Natural sciences
Sub-field of research 1.4 Chemical sciences
Authors Jekaterīna Ivanova
Vaida Morkunaite
Lina Baranauskiene
Asta Zubriene
Visvaldas Kairys
Peteris Trapencieris
Daumantas Matulis
Keywords
Abstract 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
Hyperlink: https://www.hindawi.com/journals/bmri/2014/638902/ 
Reference 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, pp.1-9. ISSN 2314-6133. Available from: doi:10.1155/2014/638902
Additional information Citation count:
ID 24037