从三链体到B型双链体稳定：氨基糖苷二聚体对靶标选择性的逆转
From triplex to B-form duplex stabilization: reversal of target selectivity by aminoglycoside dimers.
作者信息
Arya Dev P, Coffee R Lane, Xue Liang
机构信息
Laboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA.
出版信息
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4643-6. doi: 10.1016/j.bmcl.2004.07.002.
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.
氨基糖苷类已被证明可作用于A-型核酸。我们之前的工作表明，新霉素（以及其他氨基糖苷类）能结合并稳定DNA/RNA三链体和其他A-型核酸。我们在此报告氨基糖苷二聚体（新霉素-新霉素和新霉素-妥布霉素）所表现出的意外的B-型双链稳定作用。通过等温滴定量热法测定，这些二聚体对富含AT的双链具有高度选择性，并表现出高亲和力（K(a)约为10(8)M(-1)）。
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