DNA Intercalation Facilitates Efficient DNA-Targeted Covalent Binding of Phenanthriplatin.

ABSTRACT: Phenanthriplatin, a monofunctional anticancer agent derived from cisplatin, shows significantly more rapid DNA covalent-binding activity compared to its parent complex. To understand the underlying molecular mechanism, we used single-molecule studies with optical tweezers to probe the kinetics of DNA-phenanthriplatin binding as well as DNA binding to several control complexes. The time-dependent extensions of single λ-DNA molecules were monitored at constant applied forces and compound concentrations, followed by rinsing with a compound-free solution. DNA-phenanthriplatin association consisted of fast and reversible DNA lengthening with time constant τ ≈ 10 s, followed by slow and irreversible DNA elongation that reached equilibrium in ∼30 min. In contrast, only reversible fast DNA elongat

SUBMITTER: Almaqwashi AA 

PROVIDER: S-EPMC6491043 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature