کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8434118 | 1546635 | 2018 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The positive inotropic agent DPI-201106 selectively reverses ABCB1-mediated multidrug resistance in cancer cell lines
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کلمات کلیدی
ABCCCK-8MDRFCSABCB1IMDMIscove's modified Dulbecco's medium - Medculus Dulbecco اصلاح شده Iscove استMTT - MTTsodium orthovanadate - سدیم ارتوواناداتfetal calf serum - سرم گوساله جنینcell counting kit-8 - شمارش سلول کیت 8Modulator - مدولاتورMultidrug resistance - مقاومت چند داروییSodium Channel - کانال سدیمATP-binding cassette - کیت اتصال به ATP
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
تحقیقات سرطان
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The positive inotropic agent DPI-201106 selectively reverses ABCB1-mediated multidrug resistance in cancer cell lines The positive inotropic agent DPI-201106 selectively reverses ABCB1-mediated multidrug resistance in cancer cell lines](/preview/png/8434118.png)
چکیده انگلیسی
The overexpression of ABCB1 in cancer cells is a major factor contributing to the development of multidrug resistance (MDR) and treatment failure in cancer patients. Therefore, re-sensitization of MDR cancer cells to anticancer drugs remains an important aspect in chemotherapy. The progress in developing clinically applicable synthetic inhibitors of ABCB1 has been slow, mostly due to complications associated with intrinsic toxicities and unforeseen drug-drug interactions. Here, we explored the drug-repositioning approach for cancer therapy by targeting ABCB1-mediated MDR in human cancer cells. We found that DPI-201106, a positive inotropic agent, selectively inhibits the drug efflux function of ABCB1, and in doing so, re-sensitizes ABCB1-overexpressing MDR cancer cells to conventional anticancer drugs. Furthermore, the ATPase activity of ABCB1 and docking analysis of DPI-201106 in the drug-binding pocket of ABCB1 were determined to confirm the interaction between DPI-201106 and ABCB1 protein. In summary, we revealed an additional action and a potential clinical application of DPI-201106 to reverse ABCB1-mediated MDR in human cancer cells, which may be beneficial for cancer patients who have developed multidrug resistance and no longer respond to conventional chemotherapy, and should be further investigated.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Cancer Letters - Volume 434, 10 October 2018, Pages 81-90
Journal: Cancer Letters - Volume 434, 10 October 2018, Pages 81-90
نویسندگان
Sung-Han Hsiao, Megumi Murakami, Ni Yeh, Yan-Qing Li, Tai-Ho Hung, Yu-Shan Wu, Suresh V. Ambudkar, Chung-Pu Wu,