1.
Bioorg Med Chem Lett
; 19(3): 618-23, 2009 Feb 01.
Article
in English
| MEDLINE
| ID: mdl-19131243
ABSTRACT
A series of oligonucleotides with various lengths that contain nick and topoisomerase I-binding sites were designed. The interactions between these oligonucleotides and human topoisomerase I were investigated and the most efficient one among them has displayed IC(50) value of 6.3 nM. Our studies have also demonstrated that the position of the nick as well as the length of the oligonucleotides were crucial factors for the inhibition of this nuclear enzyme.
Subject(s)
Enzyme Inhibitors/pharmacology , Oligonucleotides/chemistry , Topoisomerase I Inhibitors , Base Sequence , Binding Sites , Catalysis , Cell Nucleus/enzymology , DNA/chemistry , Drug Design , Enzyme Inhibitors/chemistry , Humans , Inhibitory Concentration 50 , Models, Genetic , Molecular Sequence Data , Nucleic Acid Conformation , Substrate Specificity
2.
Bioorg Med Chem Lett
; 18(20): 5576-80, 2008 Oct 15.
Article
in English
| MEDLINE
| ID: mdl-18812258
ABSTRACT
It is demonstrated in our investigations that certain G-quadruplex structures formed by human telomeric repeats could perform self-cleaving actions. Our further studies verify that these reactions are site-specific and undergo hydrolytic pathways.
