دورية أكاديمية
The Sulfamate Small Molecule CAIX Inhibitor S4 Modulates Doxorubicin Efficacy.
العنوان: | The Sulfamate Small Molecule CAIX Inhibitor S4 Modulates Doxorubicin Efficacy. |
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المؤلفون: | Simon J A van Kuijk, Roben G Gieling, Raymon Niemans, Natasja G Lieuwes, Rianne Biemans, Brian A Telfer, Guido R M M Haenen, Ala Yaromina, Philippe Lambin, Ludwig J Dubois, Kaye J Williams |
المصدر: | PLoS ONE, Vol 11, Iss 8, p e0161040 (2016) |
بيانات النشر: | Public Library of Science (PLoS), 2016. |
سنة النشر: | 2016 |
المجموعة: | LCC:Medicine LCC:Science |
مصطلحات موضوعية: | Medicine, Science |
الوصف: | 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 its efficacy. The aim of this study was to determine if doxorubicin efficacy can be increased when combined with the selective sulfamate CAIX inhibitor S4. The effect of S4 on doxorubicin efficacy was tested in vitro using cell viability assays with MDA-MB-231, FaDu, HT29 -CAIX high and HT29 -CAIX low cell lines. In addition, the efficacy of this combination therapy was investigated in tumor xenografts of the same cell lines. The addition of S4 in vitro increased the efficacy of doxorubicin in the MDA-MB-231 during hypoxic exposure (IC50 is 0.25 versus 0.14 µM, p = 0.0003). Similar results were observed for HT29-CAIX high with S4 during normoxia (IC50 is 0.20 versus 0.08 µM, p |
نوع الوثيقة: | article |
وصف الملف: | electronic resource |
اللغة: | English |
تدمد: | 1932-6203 |
Relation: | http://europepmc.org/articles/PMC4981362?pdf=render; https://doaj.org/toc/1932-6203 |
DOI: | 10.1371/journal.pone.0161040 |
URL الوصول: | https://doaj.org/article/ac88a352ecf64264b8874d1a5184899c |
رقم الأكسشن: | edsdoj.88a352ecf64264b8874d1a5184899c |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 19326203 |
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DOI: | 10.1371/journal.pone.0161040 |