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Alkylating Agent

Alkylating agents work to add alkyl groups to negatively-charged groups. They are known to stop tumor growth through cross-linking guanine nucleobases in strands of DNA, which directly damages the DNA by making it unable to uncoil and separate. The cell, when attacked in this way, is unable to replicate. While it may not die, it also cannot grow.

Dialkylating agents react with two different guanine nucleobases; if they are in different strands of DNA, the two halves are bonded together. In the same strand, the drug molecule attaches itself to the DNA in both sites, not preventing the separation but preventing processing of critical enzymes and stimulating apoptosis. Monoalkylating agents react with only one guanine nucleobase, and may not act quite as easily.

Because alkylating agents are nonspecific in action – and can attack healthy cells as easily as tumorous ones – it is critical that the agent be applied locally, targeting the tumor.

Cyclophosphamide is one alkylating agent, and is also an immunosuppressive. It is used to treat lupus and certain autoimmune anemias, along with other autoimmune diseases.

Web Resources On Alkylating Agent

Mechanisms of Alkylating Agents
Types of Alkylating Agent

Book Resources On Alkylating Agent

Biological Alkylating Agents: Fundamental Chemistry and the Design of Compounds for Selective Toxicity by W. C. J. Ross
Biological Effects of Alkylating Agents by Benjamin L. Albertson (Ed.)

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