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An alkylating antineoplastic agent is an alkylating agent used in cancer treatment that attaches an alkyl group (C n H 2n+1) to DNA. [ 1 ] Since cancer cells, in general, proliferate faster and with less error-correcting than healthy cells, cancer cells are more sensitive to DNA damage—such as being alkylated.
Electrophilic, soluble alkylating agents are often toxic and carcinogenic, due to their tendency to alkylate DNA. This mechanism of toxicity is relevant to the function of anti-cancer drugs in the form of alkylating antineoplastic agents. Some chemical weapons such as mustard gas (sulfide of dichloroethyl) function as alkylating agents ...
Although originally produced as chemical warfare agents, [2] [3] they were the first chemotherapeutic agents for treatment of cancer. [4] Nitrogen mustards are nonspecific DNA alkylating agents . Name
The precise mechanism by which altretamine exerts its anti-cancer effect is unknown but it is classified by MeSH as an alkylating antineoplastic agent. [5] This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation. Administered ...
Alkylating agents are the oldest group of chemotherapeutics in use today. Originally derived from mustard gas used in World War I, there are now many types of alkylating agents in use. [4] They are so named because of their ability to alkylate many molecules, including proteins, RNA and DNA.
Ifosfamide is a DNA-damaging alkylating agent, belonging to the same class of chemotherapy drugs as cyclophosphamide. It is a prodrug, meaning that It has to be converted by CYP450 into its main active metabolites-(Iso)phosphoramide mustards. These metabolites form DNA cross links mainly at Guanine N-7 positions. [5]
Carmustine is used as an alkylating agent to treat several types of brain cancer including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma, multiple myeloma, and lymphoma (Hodgkin's and non-Hodgkin). Carmustine is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as O 6-benzylguanine.
Melphalan belongs to the class of nitrogen mustard alkylating agents. [7] It works by interfering with the creation of DNA and RNA. [7] Melphalan was approved for medical use in the United States in 1964. [7] It is on the World Health Organization's List of Essential Medicines. [9] It is available as a generic medication. [10]