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DNA polyintercalation: comparison of DNA binding properties of an acridine dimer and trimer
Author(s) -
Gaugain Bernard,
Markovits Judith,
Le Pecq Jean-Bernard,
Roques Bernard P.
Publication year - 1984
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(84)80302-6
Subject(s) - trimer , dna , dimer , intercalation (chemistry) , chemistry , acridine , derivative (finance) , stereochemistry , binding site , crystallography , biophysics , biochemistry , biology , organic chemistry , financial economics , economics
The DNA binding characteristics of a mono‐, di‐ and trimeric derivative of 9‐aminoacridine were studied. The length of the linking carboxyamidoalkyl chains was selected to allow bis‐ or tris‐intercalation according to the excluded‐site model. Measurements of DNA unwinding angle using closed circular DNA showed that the trimeric derivative behaves as a tris‐intercalating agent. Nevertheless the increase of DNA binding affinity on going from dimer to trimer was found to be relatively small. This is probably related to the large structural constraint for DNA binding of the trimeric derivative. The nature of the linking chain for the design of high‐affinity DNA poly‐intercalating agents appears therefore critical.

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