کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5847864 | 1561610 | 2015 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Inhibition of the insulin-like growth factor 1 receptor by CHM-1 blocks proliferation of glioblastoma multiforme cells
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کلمات کلیدی
phosphatidylinositol 3′ kinaseCHM-1PDGFRFGFRIGF-1REGFRGBMmTORPI3K3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide - 3- (4،5-dimethylthiazol-2-yl) -2،5-difenyltetrazolium bromideMAPK - MAPKMTT - MTTQuinolone derivatives - مشتقات کینولونmammalian target of rapamycin - هدف پستانداران رپامایسینmitogen-activated protein kinase - پروتئین کیناز فعال با mitogenGlioblastoma multiforme - گلیوبلاستوم مولتیفرم، گلیوبلاستوماinsulin receptor - گیرنده انسولینplatelet-derived growth factor receptor - گیرنده عامل فاکتور رشد یافته پلاکتInsulin-like growth factor-1 receptor - گیرنده فاکتور 1 رشد انسولینEpidermal growth factor receptor - گیرنده فاکتور رشد اپیدرمالfibroblast growth factor receptor - گیرنده فاکتور رشد فیبروبلاست
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم محیط زیست
بهداشت، سم شناسی و جهش زایی
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چکیده انگلیسی
The insulin-like growth factor-1 receptor (IGF-1R) plays a pivotal role in transformation, growth, and survival of glioblastoma multiforme (GBM) cells, and has emerged as a general and promising target for cancer treatment. In this study, we examined the anti-tumor effects of CHM-1, a synthetic 6,7-methylenedioxy substituted 2-phenyl-4-quinolone derivative, on GBM cells in vitro and in vivo. CHM-1 selectively blocked IGF-1R auto-phosphorylation, with an ability to distinguish between IGF-1R and related tyrosine kinase receptors, such as insulin receptor (IR), epidermal growth factor receptor (EGFR), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR). Further investigation revealed that, the phosphorylation of ERK1/2 as well as Akt was inhibited in CHM-1 treated GBM8401 cells possibly through the selective blockage of IGF-1R auto-phosphorylation. Our study also showed that p.o. treatment with the hydrophilic dihydrogen phosphate CHM-1P reduced the tumor volumes of the GBM8401 derived tumors in mouse brain and also prolonged the survival rate. The results provided potential opportunities for effective chemotherapy for GBM.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chemico-Biological Interactions - Volume 231, 25 April 2015, Pages 119-126
Journal: Chemico-Biological Interactions - Volume 231, 25 April 2015, Pages 119-126
نویسندگان
Ying-Chao Lin, Shin-Chen Hou, Chao-Ming Hung, Jia-Ni Lin, Wei-Chih Chen, Chi-Tang Ho, Sheng-Chu Kuo, Tzong-Der Way,