ArticleScientific reports2022
Picomolar fluorescent probes for compound affinity determination to carbonic anhydrase IX expressed in live cancer cells.
Article in Scientific reports, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- Achieving femtomolar affinities in structure-based drug design.European biophysics journal : EBJ · 2026Article
- Real-Time Binding Kinetics of Small Molecules to CA IX in Live Suspension Cells Using SPR Microscopy.ACS medicinal chemistry letters · 2026Article
- Di-Journal of medicinal chemistry · 2025Article
- Development of 4T1 breast cancer mouse model system for preclinical carbonic anhydrase IX studies.FEBS open bio · 2025Article
- Novel Derivatives of 3-Amino-4-hydroxy-benzenesulfonamide: Synthesis, Binding to Carbonic Anhydrases, and Activity in Cancer Cell 2D and 3D Cultures.International journal of molecular sciences · 2025Article
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- High-Affinity NIR-Fluorescent Inhibitors for Tumor Imaging via Carbonic Anhydrase IX.Bioconjugate chemistry · 2024Article
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Authors and funding
28 authors at 5 institutions in 5 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Numerous human cancers, especially hypoxic solid tumors, express carbonic anhydrase IX (CAIX), a transmembrane protein with its catalytic domain located in the extracellular space. CAIX acidifies the tumor microenvironment, promotes metastases and invasiveness, and is therefore considered a promising anticancer target. We have designed a series of high affinity and high selectivity fluorescein-labeled compounds targeting CAIX to visualize and quantify CAIX expression in cancer cells. The competitive binding model enabled the determination of common CA inhibitors' dissociation constants for CAIX expressed in exponentially growing cancer cells. All tested sulfonamide compounds bound the proliferating cells with similar affinity as to recombinantly purified CAIX. The probes are applicable for the design of selective drug-like compounds for CAIX and the competition strategy could be applied to other drug targets.
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Registered trials
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