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Beschreibung

A cell-permeable sulfonamide that selectively inhibits the growth of VHL-deficient renal cell carcinomas (RCCs) dose-dependently (0-5 µ,M) by directly targeting glucose transporter 1 (GLUT1), which is up-regulated by HIF (hypoxia-inducible factor) transcription factor in VHL-deficient cells. It elicits decreased oxidative phosphorylation associated with aerobic glycolysis and leads to necrosis, which is consistent with the effect induced by GLUT1 RNA interference. It does not bind to other glucose transporters, and does not inhibit a broad range of 50 tested kinases.