Repozytorium publikacji - Politechnika Gdańska

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.

Autorzy

• Karolina Jagiełło link otwiera się w nowej karcie ,
• Anita Dopierała,
• prof. dr hab. inż. Jan Mazerski link otwiera się w nowej karcie