What is alkylation of DNA?
What is alkylation of DNA?
DNA alkylation refers to the addition of alkyl groups to specific bases, resulting in alkylation products such as O2‐alkylthymine, O4‐alkylthymine, O6‐methylguanine and O6‐ethylguanine, which cause DNA mutations.
Which is an example of nitrosoureas derivative?
The nitrosoureas include carmustine (BCNU), lomustine (CCNU) and semustine.
What is the mechanism of action of carmustine?
Carmustine causes cross-links in DNA and RNA, leading to the inhibition of DNA synthesis, RNA production and RNA translation (protein synthesis). Carmustine also binds to and modifies (carbamoylates) glutathione reductase. This leads to cell death. Hepatic and rapid with active metabolites.
What is the action of Nitrosoureas?
The nitrosoureas BCNU, CCNU, ACNU, and Fotemustine covalently deactivate thioredoxin reductase, glutathione reductase and ribonucleotide reductase by alkylating their thiolate active sites.
Are Nitrosoureas hydrophilic?
In 1967, streptozotocin (Zanosar®), a hydrophilic natural nitrosourea, was isolated from a strain of Streptomyces achromogens.
How is carmustine administered?
Intravenous infusion: Administer the carmustine admixture as a slow IV infusion over 2 hours or longer not to exceed a rate of 1.66 mg/m2 per minute; injection-site pain and burning may occur with infusions given over less than 2 hours. NOTE: Carmustine is not approved by the FDA for topical administration.
How is carmustine given?
Carmustine is usually given by an infusion into a vein (intravenous, IV). There is no pill form of this medication. There is a form of this medication (Gliadel® wafer) that can be placed and left in the cavity after surgical removal of a brain tumor.
Which are alkylating agents?
Some examples of alkylating agents are nitrogen mustards (chlorambucil and cyclophosphamide), cisplatin, nitrosoureas (carmustine, lomustine, and semustine), alkylsulfonates (busulfan), ethyleneimines (thiotepa), and triazines (dacarbazine). …
What do you mean by alkylating agent?
Definition of alkylating agent : a substance that causes replacement of hydrogen by an alkyl group especially in a biologically important molecule specifically : one with mutagenic activity that inhibits cell division and growth and is used to treat some cancers.
