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The Sound of Evolution
Cisplatin
順鉑
Mechanism of action:
Cisplatin 是一種含鉑的具烷化反應性化合物（platinum-based alkylating-like agent）。Cisplatin 進入細胞後，受細胞內低氯離子濃度（低於血漿）的影響，兩個氯原子被水分子取代，形成活性型 [Pt(NH₃)₂(H₂O)₂]²⁺。此水合型離子（aquated complex）有著較強的親電性（electrophilic），能與 DNA 上的鹼基，特別是鳥糞嘌呤（guanine）發生共價反應，會導致 DNA 同股內交聯（intrastrand cross-link）與雙股間交聯（interstrand cross-link）。之後讓 DNA 無法進行複製與轉錄，觸發細胞的 DNA 損傷反應並啟動凋亡路徑（常涉及 p53 等途徑）。
Reference(s):
1. Garcia Sar D et al. (2008). In vivo detection of DNA adducts induced by cisplatin using capillary HPLC-ICP-MS and their correlation with genotoxic damage in Drosophila melanogaster. Anal Bioanal Chem.
2. Sharma S et al. (2007). Molecular dynamic simulations of cisplatin- and oxaliplatin-d(GG) intrastand cross-links reveal differences in their conformational dynamics. J Mol Biol.
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