Cisplatin

Cisplatin is a platinum-containing compound that acts as a DNA-crosslinking agent and interferes with replication and transcription, culminating in apoptosis.¹ It forms intra- and interstrand crosslinks with DNA with intrastrand guanine-to-guanine or guanine-to-alanine links accounting for the majority of DNA binding.² Cisplatin halts the cell cycle at the G₂/M phase in vitro and is active against murine tumors transplanted into mice and in mouse xenograft models, including a reduction in tumor growth in a model of squamous cell carcinoma of the head and neck when administered at doses ranging from 7.5 to 12.5 mg/kg.^3,4 Cisplatin also inhibits the RecA recombinase of M. tuberculosis (IC₅₀ = 2 µM), blocking protein splicing and cell growth.⁵ Formulations containing cisplatin have been used, alone and in combination therapy, in the treatment of a variety of cancers.

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1. Schmitt, S.M., Frezza, M., and Dou, Q.P. New applications of old metal-binding drugs in the treatment of human cancer. Front. Biosci. (Schol. Ed.) 4, 375-391 (2012).

2. Bose, R.N. Biomolecular targets for platinum antitumor drugs. Mini. Rev. Med. Chem. 2(2), 103-111 (2002).

3. Takahashi, K., Ebihara, K., Honda, Y., et al. Antitumor activity of cis-dichlorodiammineplatinum(II) and its effect on cell cycle progression. Gan To Kagaku Ryoho. 9(4), 624-631 (1982).

4. Wennerberg, J., Alm, P., Biörklund, A., et al. Cell cycle perturbations in heterotransplanted squamous-cell carcinoma of the head and neck after mitomycin C and Cisplatin treatment. Int. J. Cancer. 33(2), 213-222 (1984).

5. Zhang, L., Zheng, Y., Callahan, B., et al. Cisplatin inhibits protein splicing, suggesting inteins as therapeutic targets in mycobacteria. The Journal of Biological Chemisty 286(2), 1277-1282 (2011).

Kremer, D.M., Nelson, B.S., Lin, L., et al. GOT1 inhibition primes pancreatic cancer for ferroptosis through the autophagic release of labile iron. bioRxiv (2020).