Methyl 2-Halo-4-Substituted-5-Sulfamoyl-Benzoates as High Affinity and Selective Inhibitors of Carbonic Anhydrase IX

Methyl 2-Halo-4-Substituted-5-Sulfamoyl-Benzoates as High Affinity and Selective Inhibitors of Carbonic Anhydrase IX

Among the twelve catalytically active carbonic anhydrase isozymes present in the human body, the CAIX is highly overexpressed in various solid tumors. The enzyme acidifies the tumor microenvironment enabling invasion and metastatic processes. Therefore, many attempts have been made to design chemica...

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Bibliographic Details
Main Authors: Audrius Zakšauskas, Edita Čapkauskaitė, Vaida Paketurytė-Latvė, Alexey Smirnov, Janis Leitans, Andris Kazaks, Elviss Dvinskis, Laimonas Stančaitis, Aurelija Mickevičiūtė, Jelena Jachno, Linas Jezepčikas, Vaida Linkuvienė, Andrius Sakalauskas, Elena Manakova, Saulius Gražulis, Jurgita Matulienė, Kaspars Tars, Daumantas Matulis
Format: Article
Language:English
Published: MDPI AG 2021-12-01
Series:International Journal of Molecular Sciences
Subjects:
methyl 5-sulfamoyl-benzoate
human carbonic anhydrase
<i>intrinsic</i> binding thermodynamics
enzyme inhibitor
X-ray crystallography
fluorescent thermal shift assay
Online Access:https://www.mdpi.com/1422-0067/23/1/130

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