This paper reports an investigation into the impact of pyridyl functional groups in conjunction with hydroxide-substituted benzenesulfonamides on the inhibition of human carbonic anhydrase (CA; EC 4.2.1.1) enzymes. These compounds were tested in vitro of CA II and CA IX, two physiologically important CA isoforms. The most potent inhibitory molecules against CA IX, 3g, 3h, and 3k, were studied to understand their binding modes via X-ray crystallography in adduct with CA II and CA IX-mimic. This research further adds to the field of CA inhibitors to better understand ligand selectivity between isoforms found in humans.

New Insights into Conformationally Restricted Carbonic Anhydrase Inhibitors / Combs J.; Bozdag M.; Cravey L.D.; Kota A.; McKenna R.; Angeli A.; Carta F.; Supuran C.T.. - In: MOLECULES. - ISSN 1420-3049. - ELETTRONICO. - 28:(2023), pp. 890.890-890.890. [10.3390/molecules28020890]

New Insights into Conformationally Restricted Carbonic Anhydrase Inhibitors

Bozdag M.;Angeli A.;Carta F.;Supuran C. T.
2023

Abstract

This paper reports an investigation into the impact of pyridyl functional groups in conjunction with hydroxide-substituted benzenesulfonamides on the inhibition of human carbonic anhydrase (CA; EC 4.2.1.1) enzymes. These compounds were tested in vitro of CA II and CA IX, two physiologically important CA isoforms. The most potent inhibitory molecules against CA IX, 3g, 3h, and 3k, were studied to understand their binding modes via X-ray crystallography in adduct with CA II and CA IX-mimic. This research further adds to the field of CA inhibitors to better understand ligand selectivity between isoforms found in humans.
2023
28
890
890
Combs J.; Bozdag M.; Cravey L.D.; Kota A.; McKenna R.; Angeli A.; Carta F.; Supuran C.T.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1305635
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