[Overcoming of multidrug resistance by a newly synthesized quinoline compound, MS-209].
The emergence of multidrug resistance(MDR) is a major problem in cancer chemotherapy. Many compounds are developed to reverse MDR, and some of them are under clinical trials. Among them, MS-209, a novel quinoline derivative, is one of the most potent MDR reversing agents. MS-209 at 3 microM effectively reverses MDR in various cell lines in vitro. MS-209 directly interacts with P-glycoprotein and inhibits the P-glycoprotein-mediated drug transport. Oral administration of MS-209 combined with anticancer drugs markedly increases the life span of mice bearing MDR tumor cells without causing serious side effects. Thus, MS-209 is an orally active and potent MDR reversing drug without serious side effects.
Naito
M
M
Institute of Molecular and Cellular Biosciences, University of Tokyo.
Nakanishi
O
O
Tsuruo
T
T
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D011804:Quinolines / Q000008:administration & dosage / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D011804:Quinolines; C087719:dofequidar