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Elsamicin a binding to DNA. A comparative thermodynamic characterization

AuthorsBarceló, Francisca; Portugal, José
Issue Date8-Oct-2004
CitationFEBS Letters 576(1-2): 68-72 (2004)
AbstractThe antitumor drug elsamicin A contains a coumarin-related chartarin chromophore that intercalates into DNA. It differs from other related molecules in its disaccharide moiety, which bears an amino sugar. Its binding to DNA was analyzed using isothermal titration calorimetry and UV thermal denaturation, and characterized thermodynamically. For the association of elsamicin A with DNA we found ΔG°=-8.6 kcal mol-1, ΔH=-10.4 kcal mol-1, ΔS=-6.1 cal mol-1 K-1, and K obs=2.8(±0.2)×106 M-1 at 20°C in 18 mM Na+. The contributions to the free energy of binding that lead to the DNA-elsamicin complex are compared with the binding to DNA of chartreusin, another chartarin-containing drug. The results are discussed in terms of the contributions of the disaccharide moieties into the strength of binding. © 2004 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
Publisher version (URL)http://dx.doi.org/10.1016/j.febslet.2004.08.063
Identifiersdoi: 10.1016/j.febslet.2004.08.063
issn: 0014-5793
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