Carbohydrate-based inducers of cellular stress for targeting cancer cells
| Autor: | Shima Nagi, Young Hoon Ahn, Fidelis Toloyi Ndombera, Garrett C. VanHecke |
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| Rok vydání: | 2015 |
| Předmět: |
0301 basic medicine
Cell Survival Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry 03 medical and health sciences Structure-Activity Relationship 0302 clinical medicine Stress Physiological Cell Line Tumor Drug Discovery medicine Humans Glycosides Cytotoxicity Molecular Biology Cell Proliferation chemistry.chemical_classification Reactive oxygen species Dose-Response Relationship Drug Molecular Structure Chemistry Cell growth Organic Chemistry HEK 293 cells Cancer AMPK medicine.disease Cell biology 030104 developmental biology HEK293 Cells Acetylation 030220 oncology & carcinogenesis Cancer cell Molecular Medicine Reactive Oxygen Species |
| Zdroj: | Bioorganicmedicinal chemistry letters. 26(5) |
| ISSN: | 1464-3405 |
| Popis: | Small molecules that block the altered metabolism in cancer or increase the production of reactive oxygen species (ROS) are emerging as potential anti-cancer agents. Considering that various carbohydrates can be used for cellular energetics or protein N-glycosylation of which interruption can lead to cellular stress, we have synthesized and evaluated a library of N-aryl glycosides for induction of ROS and cytotoxicity in H1299 cancer cell line. Two N-aryl glycosides (K8 and H8) were identified that induce about 2-fold induction of ROS and cytotoxicity in H1299 cells. We further showed that the acetylated form of K8 (K8A) activates AMPK, and stabilizes p53 in HEK293 cells, and induce a higher cytotoxicity than 2-deoxy-d-glucose in H1299 cell line. |
| Databáze: | OpenAIRE |
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