Targeting carbonic anhydrase IX with small organic ligands
| Autor: | Nikolaus Krall, Moreno Wichert |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Antineoplastic Agents
Ligands Biochemistry Analytical Chemistry Metastasis Small Molecule Libraries Mice Antigen Antigens Neoplasm Cell Line Tumor medicine Animals Humans Cytotoxic T cell Molecular Targeted Therapy Carbonic Anhydrase IX Carbonic Anhydrase Inhibitors Carbonic Anhydrases biology medicine.disease Xenograft Model Antitumor Assays Small molecule Acetazolamide Targeted drug delivery Cell culture biology.protein Cancer research Protein Multimerization Antibody Colorectal Neoplasms Homeostasis |
| Zdroj: | Current Opinion in Chemical Biology. 26:48-54 |
| ISSN: | 1367-5931 |
| DOI: | 10.1016/j.cbpa.2015.02.005 |
| Popis: | Carbonic anhydrase IX (CAIX) is expressed in many solid tumors in response to hypoxia and plays an important role in tumor acid-base homeostasis under these conditions. It is also constitutively expressed in the majority of renal cell carcinoma. Its functional inhibition with small molecules has recently been shown to retard tumor growth in murine models of cancer, reduce metastasis and tumor stem cell expansion. Additionally, CAIX is a promising antigen for targeted drug delivery approaches. Initially validated with anti-CAIX antibodies, the tumor-homing capacity of high-affinity small-molecule ligands of CAIX has recently been demonstrated. Indeed, conjugates formed of CAIX ligands and potent cytotoxic drugs could eradicate CAIX-expressing solid tumors in mice. These results suggest that CAIX is a promising target for the development of novel therapies for the treatment of solid tumors. |
| Databáze: | OpenAIRE |
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