[Role of the functional groups of the sibiromycin molecule in DNA binding].
Biological activity of 2 derivatives of sibiromycin, an antibiotic close by its chemical structure to antramycin and their capacity for formation of complexes with DNA was studied. Anhydrosibiromycin like sibiromycin formed a complex with DNA. The antibiotic increased the DNA melting point but to a less extent than sibiromycin. Anhydrosibiromycin had a low activity in the system of DNA-dependent RNA-polymerase. The low biological activity of anhydrosibiromycin must be due to instability of the antibiotic complex with DNA. Methyl ether of sibiromycin by the phenol hydroxyl, the other derivative of sibiromycin had no biological activity and did not interact with DNA. On the basis of experimental data it was suggested that definite functional groups of the sibiromycin participated in DNA binding.
D000903:Antibiotics, Antineoplastic / Q000031:analogs & derivatives / Q000378:metabolism*; D004269:DNA, Bacterial / Q000378:metabolism*; D012321:DNA-Directed RNA Polymerases / Q000494:pharmacology; D004355:Drug Stability; D004926:Escherichia coli; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008968:Molecular Conformation; D011485:Protein Binding / Q000187:drug effects; D012967:Sodium Dodecyl Sulfate / Q000494:pharmacology; D012996:Solutions; D013053:Spectrophotometry; D013329:Structure-Activity Relationship; D013696:Temperature
D000903:Antibiotics, Antineoplastic; D004269:DNA, Bacterial; D012996:Solutions; D012967:Sodium Dodecyl Sulfate; D012321:DNA-Directed RNA Polymerases
Rol' funktsional'nykh grupp molekuly sibiromitsina v sviazyvanii s DNK.