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Quarfloxin is an inhibitor of RNA polymerase I-mediated transcription.1 It binds to G-quadruplex DNA and inhibits the interaction between ribosomal DNA G-quadruplexes and nucleolin, a nucleolar protein required for RNA polymerase I-mediated transcription. Quarfloxin (10 µM) induces nucleolin mislocalization from the nucleoli to the nucleoplasm in A549 cells. It induces apoptosis in A549 and HL-60 cells when used at a concentration of 5 µM. Quarfloxin (5 mg/kg) reduces tumor growth in MDA-MB-231 breast and MiaPaCa-2 pancreatic cancer mouse xenograft models.
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1. Anticancer activity of CX-