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KT-5720 Reverses Multidrug Resistance in Variant S49 Mouse Lymphoma Cells Transduced With the Human MDR1 cDNA and in Human Multidrug-Resistant Carcinoma Cells

KT-5720 Reverses Multidrug Resistance in Variant S49 Mouse Lymphoma Cells Transduced With the Human MDR1 cDNA and in Human Multidrug-Resistant Carcinoma Cells

H Galski, P Lazarovici, M M Gottesman, C Murakata, Y Matsuda, J Hochman

Eur J Cancer. 1995;31A(3):380-8.

PMID: 7786606

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP108068980-B	KT 5720		108068-98-0	Price

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