An Approach To Enhance Specificity against RNA Targets Using Heteroconjugates of Aminoglycosides and Chloramphenicol (or Linezolid)

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• 作者：Jongkook Lee ; Miyun Kwon ; Kyung Hyun Lee ; Sunjoo Jeong ; Soonsil Hyun ; Kye Jung Shin ; and Jaehoon Yu
• 刊名：Journal of the American Chemical Society
• 出版年：2004
• 出版时间：February 25, 2004
• 年：2004
• 卷：126
• 期：7
• 页码：1956 - 1957
• 全文大小：39K
• 年卷期：v.126,no.7(February 25, 2004)
• ISSN：1520-5126

文摘

We describe the design and synthesis of new heterodimeric conjugates, which are comprised of a neomycin B (Neo) stem-binding component and a chloramphenicol (Cam) or linezolid (Lnz) loop-binding component. Some of the heterodimeric conjugates display enhanced affinities to RNA targets and that binding occurs in both stem and loop regions of the RNA. In addition, the results of foot-printing and mutation studies suggest that the enhanced binding affinity of the conjugates is RNA sequence-specific.