NSC73306, a thiosemicarbazone, is a cell penetrant, cytotoxic agent that exhibits greater toxicity against cells expressing functional P-gp (P-glycoprotein) than against other cells.
NSC73306, a thiosemicarbazone, is a cell penetrant, cytotoxic agent that exhibits greater toxicity against cells expressing functional P-gp (P-glycoprotein) than against other cells. Irrespective of variations in cell line background, NSC73306 consistently demonstrated a Pgp-potentiated MDR-selective toxicity. It appears that NSC73306 is transported into the cell by copper transporter 1 (CTR1, SLC31A1). It is not P-gp inhibitor.
ATP-binding cassette (ABC) proteins include the best known mediators of resistance to anticancer drugs. In particular, ABCB1 [MDR1/P-glycoprotein (P-gp)] extrudes many types of drugs from cancer cells, thereby conferring resistance to those agents. Attempts to overcome P-gp-mediated drug resistance using
Oxidative medicine and cellular longevity, 2015, 394367-394367 (2015-06-16)
A series of thiosemicarbazone (TSC) p-substituted acetophenone derivatives were synthesized and chemically characterized. The p-substituents appended to the phenyl group of the TSC structures were hydrogen, fluor, chlorine, methyl, and nitro, producing compounds named TSC-H, TSC-F, TSC-Cl, TSC-Me, and TSC-NO2
Acquired drug resistance in cancer continues to be a challenge in cancer therapy, in part due to overexpression of the drug efflux transporter P-glycoprotein (P-gp, MDR1, ABCB1). NSC73306 is a thiosemicarbazone compound that displays greater toxicity against cells expressing functional
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