DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed methylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.
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OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent; OBI-3424 is a nitro-benzene prodrug of N,N’-bisethylenephosphoramidate, demonstrates in vivo efficacy against preclinical xenograft models of pediatric T-ALL.
Satraplatin (BMS-182751, BMY-45594, JM-216) is a platinum-based antineoplastic agent that binds to guanine residues in DNA, inhibits DNA replication and transcription, leads to subsequent apoptosis; shows similar cytotoxicity and pattern of cytotoxicity to cisplatin against human ovarian carcinoma cell lines (IC50=1.7 uM); shows antitumor selectivity far superior to cisplatin, carboplatin, or tetraplatin in vivo; orally active.
Trabectedin (Ecteinascidin-743, ET-743, Ecteinascidin) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata that shows remarkably anticancer activity in a variety of in vitro and in vivo systems; a DNA minor groove, guanine-specific alkylating agent; shows hign potency against ovarian carcinoma xenografts.
A nitrogen mustard alkylating agent used in the treatment of cancer.
A small molecule DNA intercalater with antineoplastic activity, does not exhibit cardiotoxicity compared with doxorubicin; induces both protein-associated DNA single-strand breaks and DNA-protein crosslinks in cancer cells.
Thio-TEPA is an alkylating agent used to treat cancer that has been previously used in the palliation of a wide variety of neoplastic diseases.
Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities; used to treat cancers and autoimmune diseases.
Evofosfamide is a potent and selective hypoxia-activated phosphoramidate DNA cross-linking mustard; selectively potent under hypoxia and stable to liver microsomes; inhibits H246 cells and HT29 cells with IC50 of 0.1 uM and 0.2 uM respectively; active in an in vivo MIA PaCa-2 pancreatic cancer orthotopic xenograft model.
Melphalan is a chemotherapy agent that acts through alkylation of the DNA nucleotide guanine, and causes linkages between strands of DNA; inhibits DNA synthesis and RNA synthesis in both dividing and non-dividing tumor cells.
Mitomycin C (Ametycine) is a chemotherapeutic antibiotic that acts as a double-stranded DNA alkylating agent.
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