Targeted anticancer pre-vinylsulfone covalent inhibitors of carbonic anhydrase IX

Targeted anticancer pre-vinylsulfone covalent inhibitors of carbonic anhydrase IX

We designed novel pre-drug compounds that transform into an active form that covalently modifies particular His residue in the active site, a difficult task to achieve, and applied to carbonic anhydrase (CAIX), a transmembrane protein, highly overexpressed in hypoxic solid tumors, important for canc...

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Main Authors: Aivaras Vaškevičius, Denis Baronas, Janis Leitans, Agnė Kvietkauskaitė, Audronė Rukšėnaitė, Elena Manakova, Zigmantas Toleikis, Algirdas Kaupinis, Andris Kazaks, Marius Gedgaudas, Aurelija Mickevičiūtė, Vaida Juozapaitienė, Helgi B Schiöth, Kristaps Jaudzems, Mindaugas Valius, Kaspars Tars, Saulius Gražulis, Franz-Josef Meyer-Almes, Jurgita Matulienė, Asta Zubrienė, Virginija Dudutienė, Daumantas Matulis
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2024-12-01
Series:eLife
Subjects:
targeted covalent inhibitors
carbonic anhydrase IX
vinylsulfone
sulfonamide
fluorescent thermal shift assay
X-ray crystallography
Online Access:https://elifesciences.org/articles/101401
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