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From triplex to B-form duplex stabilization: reversal of target selectivity by aminoglycoside dimers.

Abstract：

:Aminoglycosides have been shown to target A-form nucleic acids. Our work has previously shown that neomycin (and other aminoglycosides) bind and stabilize DNA/RNA triplexes and other A-form nucleic acids. We report herein the unexpected B-form duplex stabilization shown by aminoglycoside dimers (neomycin-neomycin and neomycin-tobramycin). The dimers are highly selective for AT rich duplexes and show high affinity (K(a) approximately 10(8)M(-1)) as determined by isothermal titration calorimetry.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Arya DP,Coffee RL Jr,Xue L

doi

10.1016/j.bmcl.2004.07.002

subject

Has Abstract

pub_date

2004-09-20 00:00:00

pages

4643-6

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)00887-X

journal_volume

14

pub_type

杂志文章

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