Reversal of Multidrug Resistance in Human Leukemia K562 by Tamolarizine, a Novel Calcium Antagonist | Zendy

Norihisa Miyake | Zendy; Ryousuke Fujita | Zendy; Masaaki Ishikawa | Zendy; Motoaki Takayanagi | Zendy; Yoshio Takayanagi | Zendy; Kenichi Sasaki | Zendy

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Reversal of Multidrug Resistance in Human Leukemia K562 by Tamolarizine, a Novel Calcium Antagonist

Author(s) -

Norihisa Miyake,

Ryousuke Fujita,

Masaaki Ishikawa,

Motoaki Takayanagi,

Yoshio Takayanagi,

Kenichi Sasaki

Publication year - 2000

Publication title -

the japanese journal of pharmacology

Language(s) - English

Resource type - Journals

eISSN - 1347-3506

pISSN - 0021-5198

DOI - 10.1254/jjp.82.265

Subject(s) - k562 cells , p glycoprotein , efflux , doxorubicin , multiple drug resistance , pharmacology , cytotoxicity , antagonist , chemistry , cell culture , in vitro , leukemia , microbiology and biotechnology , chemotherapy , biology , receptor , biochemistry , immunology , medicine , antibiotics , genetics

A new type of organic Ca2+ channel blocker, tamolarizine, was examined for its reversing effect on multidrug-resistant tumor cells. Tamolarizine synergistically potentiated the cytotoxicity of doxorubicin for doxorubicin-resistant K562 cells (K562/DXR) at a concentration of 0.1-10 microM, but had hardly any synergistic effects in the parental cell line (K562) at the same concentration. Moreover, tamolarizine inhibits the P-glycoprotein pump-efflux activity in a dose-related manner and reduces the expression of the immunoreactive P-glycoprotein in K562/DXR cells as evaluated by cytofluorimetric assay. These results indicate that tamolarizine reverses the multidrug-resistance phenotype through direct interaction with P-glycoprotein.

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