Alkylated DNA (with blood-brain barrier crossing effects)

The entry "Alkylation of DNA including crossing blood-brain barrier effects" does not refer to a specific molecular target such as a receptor, enzyme, or transporter. Instead, it describes a chemical process—DNA alkylation—whereby certain drugs introduce alkyl groups onto nucleobases within the DNA molecule. This modification can result in cytotoxicity by blocking replication and transcription through the formation of adducts or cross-links. Some chemotherapeutic agents that act via this mechanism are designed to cross the blood-brain barrier for treatment of central nervous system tumors; examples include temozolomide and DM-CHOC-PEN. The effectiveness and safety profile depend on both drug properties (such as ability to penetrate the CNS) and cellular factors like expression levels of repair enzymes such as MGMT. Because this is not a discrete protein or gene product but rather a class effect/mechanism involving many possible sites on the genome—and because it refers partly to pharmacokinetic properties—it is not considered an individual therapeutic target.[1][2][3]

Other names

DNA alkylationalkylated DNA lesionsDNA cross-linking (by alkylating agents)

Alkylation of guanine and cytosine bases in DNA, leading to formation of cross-links or methylated adducts that block replication and transcription[1][2][3]