Zsila, Ferenc (2015) Glycosaminoglycans are potential pharmacological targets for classic DNA minor groove binder drugs berenil and pentamidine. PHYSICAL CHEMISTRY CHEMICAL PHYSICS, 17 (38). pp. 24560-24565. ISSN 1463-9076
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Abstract
It is shown that the antiprotozoal drugs berenil and pentamidine, conventional minor groove binders of DNA, form non-covalent complexes with polyanionic glycosaminoglycans. Induced circular dichroism (CD) spectra as well as UV hypochromism confirmed drug binding to the asymmetric template of heparin and chondroitin 6-sulfate. The biphasic nature of the CD signals refers to intermolecular chiral exciton coupling between the dicationic guest molecules forming a right- or a left-handed helical array along the GAG chains. Quantitative evaluation of the spectroscopic data measured in pH 7.0 buffer solution (80 mM NaCl) indicated a higher (Ka ∼ 106 M-1 for berenil) and a lower (Ka ∼ 105 M-1 for pentamidine) affinity heparin binding of these agents, similar to that reported for DNA. Drug-chondroitin sulfate complexes (Ka ∼ 104-105 M-1) could be detected only at low ionic strength. These results imply that besides nucleic acids, GAGs may be another pharmacological targets for diarylamidine drugs.
Item Type: | Article |
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Subjects: | Q Science / természettudomány > QD Chemistry / kémia |
SWORD Depositor: | MTMT SWORD |
Depositing User: | MTMT SWORD |
Date Deposited: | 10 Dec 2015 13:46 |
Last Modified: | 31 Aug 2016 23:15 |
URI: | http://real.mtak.hu/id/eprint/30888 |
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