Thermodynamics aspects of interactions between acridine derivatives and DNA

Karolina Jagiełło; Anita Dopierała; Jan Mazerski

Thermodynamics aspects of interactions between acridine derivatives and DNA

Abstract

DNA is a molecular target for many anticancer and antiviral drugs. Therefore, a clear understanding of the interaction of small molecules with DNA is important in the rational design of ligands that can bind to DNA with high affinity and selectivity. There are several methods to investigate interactions between drug and DNA. Some of them measure changing into DNA structures, such as lengthening and untwisting of helix of DNA. Other techniques measure changing in drug environment. With the increasing availability of sensitive microcalorimeters, particular interest has arisen in the thermodynamics of drug-DNA interaction. Isothermal titration calorimetry (ITC) permits direct determination of enthalpy changes associated with reactions. One experiment permits to obtain also binding constant, hence an almost complete thermodynamic profile can be established. This profile offers key insights into the molecular forces that drive complex formation and permit to estimate which kind of interaction are responsible of forming these complexes. Acridine derivatives are a medical important compounds with anticancer activity. DNA binding is shown to be crucial in their mode of action. ITC technique was used the first time to analyze the thermodynamics profiles on the interaction of some acridines and natural calf thymus DNA and three synthetic DNAs of differing base pair sequences under various environmental conditions. Knowledge of the DNA interactions of acridines should be useful in the rational design of new derivatives with improve properties for control of gene expression.

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Category:: Conference activity
Type:: publikacja w wydawnictwie zbiorowym recenzowanym (także w materiałach konferencyjnych)
Title of issue:: 13th International Symposium of Students and Young Mechanical Engineers : Advances in Chemical and Mechanical Engineering, Gdańsk, 20th-22nd May 2010 strony 161 - 176
Language:: English
Publication year:: 2010
Bibliographic description:: Jagiełło K., Dopierała A., Mazerski J.: Thermodynamics aspects of interactions between acridine derivatives and DNA// 13th International Symposium of Students and Young Mechanical Engineers : Advances in Chemical and Mechanical Engineering, Gdańsk, 20th-22nd May 2010/ ed. ed. C. Fijało. - Gdansk University of Technology. Gdańsk: GUT, 2010, s.161-176
Verified by:: Gdańsk University of Technology