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The Sound of Evolution
Melphalan
Mechanism of action:
Melphalan is an alkylating agent and a nitrogen mustard derivative. In the body, Melphalan forms a highly reactive aziridinium ion that binds to the N7 position of guanine in DNA. This causes DNA monoalkylation as well as interstrand and intrastrand crosslinking, preventing proper DNA unwinding and replication and ultimately impairing normal cell division.
Reference(s):
1. Loeber R et al. (2008). Cross-linking of the DNA repair protein Omicron6-alkylguanine DNA alkyltransferase to DNA in the presence of antitumor nitrogen mustards. Chem Res Toxicol.
2. Povirk LF et al. (1994). DNA damage and mutagenesis induced by nitrogen mustards. Mutat Res.
3. Lawley PD et al. (1996). DNA adducts from chemotherapeutic agents. Mutat Res.
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