کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584327 | 981329 | 2014 | 47 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3)
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کلمات کلیدی
BCARIPAECARPFK-1PFKFB3F6P6-Phosphofructo-1-kinase - 6-فسفوفروتو-1-کینازbicinchoninic acid assay - آزمون اسید بیستینکونینیکWarburg effect - اثر واربورگTEMPO - زمانradioimmunoprecipitation assay - سنجش radioimmunoprecipitationfructose-6-phosphate - فروکتوز 6-فسفاتfructose-1,6-bisphosphate - فروکتوز-1،6-بیسفسفاتFructose-2,6-bisphosphate - فروکتوز-2،6-بیسفسفاتextracellular acidification rate - نرخ اسیدی شدن خارج سلولیPyridazinone - پیریدازینونGlycolysis - گلیکولیز یا قندکافت
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
High-throughput screening of a small-molecule library identified a 5-triazolo-2-arylpyridazinone as a novel inhibitor of the important glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Such inhibitors are of interest due to PFKFB3's control of the important glycolytic pathway used by cancer cells to generate ATP. A series of analogues was synthesized to study structure-activity relationships key to enzyme inhibition. Changes to the triazolo or pyridazinone rings were not favoured, but limited-size substitutions on the aryl ring provided modest increases in potency against the enzyme. Selected analogues and literature-described inhibitors were evaluated for their ability to suppress the glycolytic pathway, as detected by a decrease in lactate production, but none of these compounds demonstrated such suppression at non-cytotoxic concentrations.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 3, 1 February 2014, Pages 1029-1039
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 3, 1 February 2014, Pages 1029-1039
نویسندگان
Darby G. Brooke, Ellen M. van Dam, Colin K.W. Watts, Amanda Khoury, Marie A. Dziadek, Hilary Brooks, Lisa-Jane K. Graham, Jack U. Flanagan, William A. Denny,