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The Sulfamate Small Molecule CAIX Inhibitor S4 Modulates Doxorubicin Efficacy.

التفاصيل البيبلوغرافية
العنوان: The Sulfamate Small Molecule CAIX Inhibitor S4 Modulates Doxorubicin Efficacy.
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
الوصف
تدمد:19326203
DOI:10.1371/journal.pone.0161040