title: A bifunctional organometallic ruthenium drug with multiple modes of inducing apoptosis.
abstract: The organometallic glutathione S-transferase inhibitor ruthenium(II) (ethacrynic acid-η(6)-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.
authors: Department of Environmental Science, University of Kalyani, India.
authors: Soumya
authors: S
authors: Chatterjee
authors: Ilaria
authors: I
authors: Biondi
authors: Paul J
authors: PJ
authors: Dyson
authors: Arindam
authors: A
authors: Bhattacharyya
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm; D005260:Female; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors; D006801:Humans; D008928:Mitochondria / Q000187:drug effects; D009942:Organometallic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism; D017975:Ruthenium Compounds / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D017382:Reactive Oxygen Species; D017975:Ruthenium Compounds; D005982:Glutathione Transferase; D002945:Cisplatin