Interactions of antitumor drug ditercalinium with nucleic acids in solutions and in situ.
Ditercalinium (7-H-pyridocarbazole dimer), a prospective antitumor drug, is a bis-intercalator characterized by a very high affinity towards nucleic acids. Specificity of binding of this drug has been studied using spectroscopy and flow cytometry. The competition experiments between the drug and 4',6-diamidino-2-phenylindole.2HCl (DAPI) or acridine orange indicate that in solution the drug had higher affinity to DNA whereas in situ it binds preferentially to RNA. The results suggest that despite their high affinity towards DNA, the intracellular target of some intercalating drugs may be RNA.
Kapuscinski
J
J
Sloan-Kettering Institute for Cancer Research, Walker Laboratory, Rye, NY 10580.
Traganos
F
F
Darzynkiewicz
Z
Z
D000970:Antineoplastic Agents; D002227:Carbazoles / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007364:Intercalating Agents; D009690:Nucleic Acid Conformation / Q000187:drug effects; D009696:Nucleic Acids / Q000378:metabolism; D012996:Solutions; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002227:Carbazoles; D007364:Intercalating Agents; D009696:Nucleic Acids; D012996:Solutions; C042804:ditercalinium