The Sulfamate Small Molecule CAIX Inhibitor S4 Modulates Doxorubicin Efficacy

• Published in: PloS one Vol. 11; no. 8; p. e0161040
• Main Authors: van Kuijk, Simon J. A., Gieling, Roben G., Niemans, Raymon, Lieuwes, Natasja G., Biemans, Rianne, Telfer, Brian A., Haenen, Guido R. M. M., Yaromina, Ala, Lambin, Philippe, Dubois, Ludwig J., Williams, Kaye J.
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 11.08.2016; Public Library of Science (PLoS)
• Subjects: Acidification; Analysis; Animals; Antibiotics, Antineoplastic - pharmacology; Biology and Life Sciences; Biotechnology; Breast cancer; Breast Neoplasms - drug therapy; Breast Neoplasms - enzymology; Breast Neoplasms - pathology; Cancer therapies; Carbon dioxide; Carbonic anhydrase; Carbonic anhydrase inhibitors; Carbonic Anhydrase Inhibitors - pharmacology; Carbonic Anhydrase IX - antagonists & inhibitors; Carbonic anhydrases; Cell Hypoxia - drug effects; Cell Proliferation - drug effects; Chemotherapy; Combination drug therapy; Dosage and administration; Doxorubicin; Doxorubicin - pharmacology; Drug therapy; Effectiveness; Female; Gene expression; Gene Expression Regulation, Neoplastic - drug effects; HT29 Cells; Humans; Hypoxia; Inhibitors; Medicine and Health Sciences; Metabolism; Metastasis; Mice; Mice, Nude; pH effects; Phenylurea Compounds - pharmacology; Physical Sciences; Proteins; Radiation therapy; Research and analysis methods; Sulfonamides - pharmacology; Treatment outcome; Tumor Cells, Cultured; Tumors; Vascular endothelial growth factor; Xenograft Model Antitumor Assays; Xenografts
• ISSN: 1932-6203; 1932-6203
• DOI: 10.1371/journal.pone.0161040

Carbonic anhydrase IX (CAIX) is a tumor-specific protein that is upregulated during hypoxic conditions where it is involved in maintaining the pH balance. CAIX causes extracellular acidification, thereby limiting the uptake of weak basic chemotherapeutic agents, such as doxorubicin, and decreasing i...