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.
Keywords: Chemotherapeutics ; Bioorganometallic chemistry ; Mitochondria ; Ruthenium ; Reactive oxygen species ; S-Transferase P1-1 ; Anticancer Drugs ; In-Vitro ; Preclinical Development ; Carcinoma-Cells ; Serum-Proteins ; Breast-Cancer ; Phase-I ; Glutathione ; Complexes
Record created on 2011-06-07, modified on 2016-08-09