A novel dicationic polyamide ligand binds in the DNA minor groove as a dimer

We have investigated DNA binding properties of a dicationic polyamide molecule (GL020924) that has exhibited unique protein displacement and gene regulation activities. Fluorescence, thermal melting and electrospray ionization mass spectrometry experiments showed that the binding stoichiometry of GL...

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Bibliographic Details
Published in:FEBS letters 2001-11, Vol.509 (1), p.85-89
Main Authors: Zhang, Wentao, Dai, Yuqin, Schmitz, Uli, Bruice, Thomas W.
Format: Article
Language:English
Subjects:
Binding stoichiometry
Cations
CD, circular dichroism
Circular Dichroism
Dimerization
DNA - chemistry
DNA - metabolism
Electrospray ionization mass spectrometry
ESI-MS, electrospray ionization mass spectrometry
HSA, hybridization stabilization assay
Ligands
Minor groove binder
Models, Chemical
Models, Molecular
Nucleic Acid Conformation
ODN, oligodeoxynucleotide
Oligopeptides - pharmacology
Protein Binding
Spectrometry, Fluorescence
Spectrometry, Mass, Electrospray Ionization
Temperature
Ultraviolet Rays
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Summary:We have investigated DNA binding properties of a dicationic polyamide molecule (GL020924) that has exhibited unique protein displacement and gene regulation activities. Fluorescence, thermal melting and electrospray ionization mass spectrometry experiments showed that the binding stoichiometry of GL020924 is 2:1 to various DNA oligomers with 8–11 contiguous A/T bp. In accordance with those findings, circular dichroism experiments showed GL020924 binds as a partially staggered side-by-side dimer spanning 10–12 bp. These observations and molecular modeling studies demonstrate that the 2:1 GL020924–DNA complex may exhibit a novel form of stacking orientation involving at least partially parallel peptide groups.
ISSN:0014-5793
1873-3468
DOI:10.1016/S0014-5793(01)03085-X