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Rhodacyanine Dye MKT-077 Inhibits in Vitro Telomerase Assay but Has No Detectable Effects on Telomerase Activity in Vivo

Renu Wadhwa, Lorel Colgin, Tomoko Yaguchi, Kazunari Taira, Roger R Reddel, Sunil C Kaul

Cancer Res. 2002 Aug 1;62(15):4434-8.

PMID: 12154051

Abstract:

MKT-077, a cationic rhodacyanine dye analogue, causes selective toxicity to cancer cells. Its cellular targets elucidated thus far include oncogenic Ras, F-actin, mortalin (hmot-2)/mthsp70, and telomerase. Here we report that MKT-077 causes growth arrest of cancer cells in culture independent of their Ras, p53, or telomerase status. Telomerase activity is inhibited in vitro by MKT-077 in the telomerase assay used. However, the in vivo toxicity seen in telomerase-positive cancer cells was not accompanied by inhibition of telomerase activity or telomere shortening. Furthermore, cells with an alternative mechanism for lengthening of telomeres were also sensitive to MKT-077 and showed enhanced formation of alternative mechanism for lengthening of telomeres-associated PML bodies in their nuclei. The data suggested that inhibition of telomerase activity is unlikely to be a prime cause of MKT-077-induced toxicity in cancer cells.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP147366414 MKT-077 MKT-077 147366-41-4 Price
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