Cisplatin (cis-diammineplatinum(II) dichloride, or cis-[Pt(NH3)2Cl2, is a potent anti-tumor agent and is active against several types of solid tumors.
It is a square planer coordination complex of platinum that was discovered in 1845 by Italian chemist Michele Peyrone and was known as Peyrone's salt. The structure was elucidated in 1993 by Alfred Werner. The prefix cis means the cis isomer in which two similar ligands are adjacent. The ammine indicates an ammonia (NH3) ligand.
The 1965, researchers at Michigan State Univ. discovered that electrolysis of platinum electrodes generated a solubl platinum complex. This led to observation that this complex could regress sarcomas in rats. It ultimately It interferes with DNA replication.
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| Mechanism of Action | Cisplatin interacts with DNA and forms intrastrand crosslink adducts which activate anti-tumor proteins ATR, p73, p53, and MAPK. Cisplatin crosslinks DNA in many ways, interfering with cell division via mitosis. DNA repair mechanisms are activated, which in turn activate apoptosis when repair is found to be impossible. Apoptosisi in human colon cancer cells depended on the mitochondrial serine-protease (Omi/Htra2). Among the other changes in DNA are cross-links with purine bases. |
| Cancer Applications |
Chemotherapeutic activity with Cisplatin responsiveness is high however resistance will eventually build up. Resistance mechanisms have been proposed: 1) changes in cellular uptake/efflux, increased detoxification, apoptosis inhibition, increased DNA repair, or metabolic changes. Paclitaxel may be used to combat Cisplatin resistance via an unknown mechanism. Cisplatin analog is carboplatin and these are common antitumor compounds. Transplatin is the trans-stereoisomer of Cisplatin, and has reduced anticancer effect. New forms of Cisplatin prodrugs can be used in combination with nanomaterials. |
| Molecular Formula | Cl2H6N2Pt |
| References | Siddik, Zahid H. "Cisplatin: Mode of Cytotoxic Action and Molecular Basis of Resistance." Oncogene 22.47 (2003): 7265-279. |