A bifunctional organometallic ruthenium drug with multiple modes of inducing apoptosis

The organometallic glutathione S-transferase inhibitor ruthenium(II) (ethacrynic acid-η6-benzylamide)(1,3,5-triaza-7-phosphaadamantane) dichloride, termed ethaRAPTA, has been demonstrated to induce apoptosis in the cisplatin-resistant MCF-7 breast cancer cell line. Probing the molecular basis of this activity suggests that the complex triggers multiple pathways toward apoptosis, including those involving endonuclease G, caspases, and c-Jun N-terminal kinase, which could provide a therapy for multi-drug-resistant tumors. Furthermore, the induction of heat shock protein 70 expression enhances selectivity of the complex for tumor cells, reducing the general toxicity. © 2011 SBIC.


Published in:
Journal of Biological Inorganic Chemistry, 16, 715-724
Year:
2011
Keywords:
Laboratories:




 Record created 2011-06-07, last modified 2018-01-28


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