KT-5720 reverses multidrug resistance in variant S49 mouse lymphoma cells transduced with the human MDR1 cDNA and in human multidrug-resistant carcinoma cells
| Autor: | Philip Lazarovici, H. Galski, C. Murakata, Jacob Hochman, Y. Matsuda, M.M. Gottesman |
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| Rok vydání: | 1995 |
| Předmět: |
Cancer Research
DNA Complementary Indoles Lymphoma Carbazoles MAP2K7 Mice Transduction Genetic Tumor Cells Cultured Animals Humans Pyrroles c-Raf ATP Binding Cassette Transporter Subfamily B Member 1 Protein kinase A Protein Kinase C P-glycoprotein biology Cyclin-dependent kinase 4 Cyclin-dependent kinase 2 Carcinoma Protein kinase R Molecular biology Drug Resistance Multiple Anti-Bacterial Agents Blotting Southern Oncology biology.protein Cyclin-dependent kinase 9 |
| Zdroj: | European journal of cancer (Oxford, England : 1990). (3) |
| ISSN: | 0959-8049 |
| Popis: | T-25-Adh cells, cell variants derived from S49 mouse lymphoma, were transduced with a retrovirus containing the human MDR1 cDNA. The resultant cells (HU-1) are cross-resistant to colchicine, doxorubicin, vinblastine and actinomycin D, and their resistance to colchicine is reversed by verapamil. HU-1 cells were used to screen several protein kinase modulators for their ability to reverse multidrug resistance. Among the tested indole carbazole (K-252a) family of protein kinase inhibitors, only the antibiotic alkaloid KT-5720 (9-n-hexyl derivative of K-252a) could overcome the multidrug resistance of HU-1 cells and KB-V1 human carcinoma cells. Since other protein kinase A, C and G modulators did not reverse multidrug resistance in the tested multidrug-resistant cells, the chemosensitising activity of KT-5720 on these cells is apparently independent of its kinase inhibitory effects. Since KT-5720 fully reversed multidrug resistance at non-toxic concentrations, it might be a candidate for clinical chemosensitisation in combination chemotherapy. |
| Databáze: | OpenAIRE |
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