A Water-Soluble Tetraazaperopyrene Dye as Strong G-Quadruplex DNA Binder.

ABSTRACT: The interactions of the water-soluble tetraazaperopyrene dye 1 with ct-DNA, duplex-[(dAdT)12 ⋅(dAdT)12 ], duplex-[(dGdC)12 ⋅(dGdC)12 ] as well as with two G-quadruplex-forming sequences, namely the human telomeric 22AG and the promotor sequence c-myc, were investigated by means of UV/visible and fluorescence spectroscopy, isothermal titration calorimetry (ITC) and molecular docking studies. Dye 1 exhibits a high affinity for G-quadruplex structures over duplex DNA structures. Furthermore, the ligand shows promising G-quadruplex discrimination, with an affinity towards c-myc of 2×10(7)  m(-1) (i.e., Kd =50 nm), which is higher than for 22AG (4×10(6)  m(-1) ). The ITC data reveal that compound 1 interacts with c-myc in a stoichiometric ratio of 1:1 but also indicate the presence of two ident

SUBMITTER: Hahn L 

PROVIDER: S-EPMC5071672 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature