Quarfloxin(CX3543)是一种具有抗肿瘤活性的氟喹诺酮类衍生物，其靶向抑制RNApolI的活性，在神经母细胞瘤中的IC50值在纳摩尔级别。Quarfloxin干扰核糖体DNA中核蛋白与G-四重DNA结构的相互作用。
Quarfloxin (CX 3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template[1].
Quarfloxin (CX 3543) effectively inhibits the growth of neuroblastoma cells in vitro. MNA (or high c-Myc) and wt-TP53 cell lines are found to be more sensitive to Quarfloxin. Quarfloxin and induces DNA damage, p53 signaling, cell death, and cell cycle arrest in neuroblastoma cell lines[1].
[1]. Hald ?H, et al. Inhibitors of ribosome biogenesis repress the growth of MYCN-amplified neuroblastoma. Oncogene. 2018 Dec 12.
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