Chan Chemical Synthetic Lethality Targeting GLUT 1 and the Warburg Effect in Renal Cell Carcinoma by

semanticscholar(2011)

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promising drug likely will bring tumor thriving to a halt. readily applied to humans to test the drug's efficacy. If it can thwart the fuel supply line in human cancers, this an approach that can be −− glucose metabolism forced on tumors by STF-31 was detected in mice with this method Glucose uptake in a tumor can be monitored by fluorodeoxyglucose positron emission tomography. The reduction in An extra benefit of the new agent is that its activity can be easily visualized, even deep inside an animal. -triphosphate production and succumbed to necrosis. ′ adenosine 5 deprived cancer cells ceased glycolysis and thus − their sugar delivery system stymied, the tumor suppressor to the transporter, STF-31 blocked glucose uptake in VHL-deficient cancer cells but not in those with intact VHL; with . By binding directly GLUT1 encoding gene − genes involved in glucose metabolism, including the glucose transporter VHL increases the activity of hypoxia-inducible factor transcription factor, which in turn stimulates the transcription of drugs, did not induce autophagy, apoptosis, or DNA damage. Rather, STF-31 exploited the fact that inactivation of identified by the authors, STF-31, was toxic to the VHL-deficient kidney tumor cells but, unlike many other cancer rather than the more typical oxidative phosphorylation for a supply of energy. The drug −− of glucose to lactate the conversion −− deficiency reorients carbohydrate metabolism so that the cancer cells depend on aerobic glycolysis Lindau (VHL) tumor suppressor protein. This − Certain kidney and other types of cancer cells lack the von Hippel in animals. class of drug that inhibits the glucose transporter and selectively impairs growth of these cancer cells in cultures and some kidney cancer cells depend on glucose for survival. By screening 64,000 small molecules, the authors found a . devised a drug discovery assay that took advantage of the fact that et al can bring proliferation to a standstill. Chan A quick tug on a fuel line can stop a car dead in its tracks. Similarly, depriving a cancer cell of its energy source Cancer's Achilles' Heel
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