Article
Spectroscopic study on the binding of a cationic porphyrin to DNA G-quadruplex under different K+ concentrations.
School of Life Science and Technology, Beijing Institute of Technology, Beijing, 100081, China.
Photochemical and Photobiological Sciences (impact factor:
2.58).
09/2008;
7(8):948-55.
DOI:10.1039/b809322a
pp.948-55
Source: PubMed
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Citations (0)
- Cited In (2)
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Article: Energetics of Ligand Binding to G-Quadruplexes.
[show abstract] [hide abstract]
ABSTRACT: G-quadruplex ligands are potential anticancer agents as telomerase inhibitors and potential transcriptional regulators of oncogenes. The search for best-in-class drugs is addressed to identify small molecules able to promote and stabilize G-quadruplex structures. What features should the G-quadruplex ligands possess? They should have selective antiproliferative effects on cancer cells and induce telomerase inhibition or oncogene suppression. One of the main challenges in their design and synthesis is to make the ligands selective for G-quadruplex DNA. These features should be amplified by careful analyses of physico-chemical aspects of G-quadruplex-drug interactions. In particular, the study of the energetics of G-quadruplex-drug interactions can enhance drug design by providing thermodynamic parameters that give quantitative information on the biomolecular interactions important for binding. The main methodologies used to gain information on energetics of binding are based on spectroscopic or calorimetric principles. Spectroscopic techniques such as fluorescence and circular dichroism are rapid and cheap methods, but are not sufficient to characterize completely the thermodynamics of interaction. Calorimetric techniques such as isothermal titration calorimetry offer a direct measure of binding enthalpy, in addition to the stoichiometry and affinity constants. With the complete thermodynamic signature of drug-target interaction, dissecting the enthalpic and entropic components of binding is possible, which can be a useful aid to decision-making during drug optimization.Topics in current chemistry 08/2012; · 4.29 Impact Factor -
Article: Applications of isothermal titration calorimetry in biophysical studies of G-quadruplexes.
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ABSTRACT: G-quadruplexes are higher-order nucleic acids structures formed by G-rich sequences that are stabilized by tetrads of hydrogen-bonded guanine bases. Recently, there has been growing interest in the study of G-quadruplexes because of their possible involvement in many biological processes. Isothermal titration calorimetry (ITC) has been proven to be a useful tool to study the energetic aspects of G-quadruplex interactions. Particularly, ITC has been applied many times to determine the thermodynamic properties of drug-quadruplex interactions to screening among various drugs and to address drug design. In the present review, we will focus on the ITC studies of G-quadruplex structures and their interaction with proteins and drugs and the most significant results will be discussed.International Journal of Molecular Sciences 07/2009; 10(7):2935-57. · 2.60 Impact Factor
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Keywords
anti-parallel
anti-parallel G4
anti-parallel G4 structure
binding reaction
cationic meso-tetrakis(4-(N-methylpyridiumyl))porphyrin
conformational conversion
different potassium ion
G-quadruplex
G4 structure
human telomeric single-strand oligonucleotide d[TAGGG(TTAGGG)3T]
K+ concentration
single-strand oligonucleotide S24
special effort
systematic spectroscopic titrations
three cases
time-resolved fluorescence spectroscopy
TMPyP4-G4 binding stoichiometry
TMPyP4-G4 complex
TMPyP4-to-G4 molar ratio