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Publication Type
Journal Article
UWI Author(s)
Author, Analytic
Arya, D.P.; Xue, L.; Tennant, Paula F.
Author Affiliation, Ana.
Department of Life Sciences
Article Title
Combining the best in triplex recognition: Synthesis and nucleic acid binding of a BQQ-neomycin conjugate
Medium Designator
n/a
Connective Phrase
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Journal Title
Journal of the American Chemical Society
Translated Title
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Reprint Status
n/a
Date of Publication
2003
Volume ID
125
Issue ID
27
Page(s)
8070-8071
Language
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Connective Phrase
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Location/URL
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ISSN
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Notes
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Abstract
Synthesis of a BQQ-neomycin conjugate is reported. The conjugate combines two ligands, one known to intercalate triplexes (BQQ) and another known to bind in the triplex groove (neomycin). The conjugate stabilizes TAT, as well as mixed base DNA triplex, better than neomycin, BQQ, or a combination of both. The conjugate selectively stabilizes the triplex (in the presence of physiological salt concentrations), with as little as 4 M of the ligand leading to a TC. Competition dialysis studies show a clear preference for the drug binding to triplex DNA/RNA over the duplex/single strand structures. Modeling studies suggest a structure of neomycin bound to the larger W-H (Watson-Hoogsteen) groove with BQQ intercalated between the triplex bases.....
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