Modification of C-seco taxoids through ring tethering and substituent replacement leading to effective agents against tumor drug resistance mediated by βIII-Tubulin and P-glycoprotein (P-gp) overexpressions
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چکیده
منابع مشابه
Co-treatment by docetaxel and vinblastine breaks down P-glycoprotein mediated chemo-resistance
Objective(s): Chemoresistance remains the main causes of treatment failure and mortality in cancer patients. There is an urgent need to investigate novel approaches to improve current therapeutic modalities and increase cancer patients' survival. Induction of drug efflux due to overexpression of P-glycoproteins is considered as an important leading cause of multidrug resistance...
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2. ABSTRACT More than 20 million epileptics worldwide do not respond to antiepileptic drugs. This is in part due to overexpression of the drug efflux transporter, P-glycoprotein, in capillaries of the blood-brain barrier. However, the mechanism signaling P-glycoprotein upregulation is unknown. Lack of this knowledge is an important clinical problem, because it limits successful treatment of pat...
متن کاملco-treatment by docetaxel and vinblastine breaks down p-glycoprotein mediated chemo-resistance
objective(s): chemoresistance remains the main causes of treatment failure and mortality in cancer patients. there is an urgent need to investigate novel approaches to improve current therapeutic modalities and increase cancer patients' survival. induction of drug efflux due to overexpression of p-glycoproteins is considered as an important leading cause of multidrug resis...
متن کاملBromocriptine reverses P-glycoprotein-mediated multidrug resistance in tumor cells.
One of the most important causes of anticancer treatment failure is the development of multidrug resistance (MDR). The main characteristics of tumor cells displaying the MDR phenomena are cross-resistance to structurally unrelated cytotoxic drugs having different mechanisms of action and the overexpression of the MDR1 gene, which encodes a transmembrane glycoprotein named P-glycoprotein (P-gp)....
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ABCB1 (P-glycoprotein, ABCB1/MDR1) is one of the major members of the ABC transporters linked to MDR in cancer cells. In this study, we observed that pristimerin, a natural triterpenoid, potently decreased P-gp in a dose-dependent manner in both drug-resistant KBv200 and stable transfected HEK293/ABCB1 cell lines. Moreover, pristimerin also inhibited cell proliferation and induced apoptosis in ...
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ژورنال
عنوان ژورنال: European Journal of Medicinal Chemistry
سال: 2017
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2017.06.001