靶向 C-myc G-四链体：通过具有不同连接长度的氨基糖-双苯并咪唑的双重识别。
Targeting C-myc G-quadruplex: dual recognition by aminosugar-bisbenzimidazoles with varying linker lengths.
机构信息
Laboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, SC 29634, USA.
出版信息
Molecules. 2013 Nov 18;18(11):14228-40. doi: 10.3390/molecules181114228.
Abstract
G-quadruplexes are therapeutically important biological targets. In this report, we present biophysical studies of neomycin-Hoechst 33258 conjugates binding to a G-quadruplex derived from the C-myc promoter sequence. Our studies indicate that conjugation of neomycin to a G-quadruplex binder, Hoechst 33258, enhances its binding. The enhancement in G-quadruplex binding of these conjugates varies with the length and composition of the linkers joining the neomycin and Hoechst 33258 units.
摘要
G-四链体是治疗学上重要的生物靶点。在本报告中，我们介绍了新霉素- Hoechst 33258 缀合物与源自 c-myc 启动子序列的 G-四链体结合的生物物理研究。我们的研究表明，将新霉素与 G-四链体结合物 Hoechst 33258 缀合可增强其结合。这些缀合物与 G-四链体的结合增强随连接新霉素和 Hoechst 33258 单元的接头的长度和组成而变化。
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