Carbocyclic analogues of lexitropsin--DNA affinity and endonuclease inhibition

Autor: Anna, Pućkowska, Danuta, Drozdowska, Krystyna, Midura-Nowaczek
Rok vydání: 2007
Předmět:
Zdroj: Acta poloniae pharmaceutica. 64(2)
ISSN: 0001-6837
Popis: A DNA-binding affinity and the effect on restriction enzymes activity of seven carbocyclic mono- and bis-lexitropsins and two analogues of pentamidine with unsubstituted N-terminal amine group were investigated. DNA association constants (Kapp) show that DNA affinity of mono-compounds is much weaker than netropsin and distamycin. Bis-analogues of netropsin bind DNA more strongly than mono-ligands, but without sequence-selectivity. Only pentamidine derivatives reveal preference to AT-rich sequence. The studied compounds can inhibit catalytical action of endonucleases recognizing sequence of four AT base pairs following one another.
Databáze: OpenAIRE