An Approach To Enhance Specificity against RNA Targets Using Heteroconjugates of Aminoglycosides and Chloramphenicol (or Linezolid)
作者:Jongkook Lee、Miyun Kwon、Kyung Hyun Lee、Sunjoo Jeong、Soonsil Hyun、Kye Jung Shin、Jaehoon Yu
DOI:10.1021/ja038937y
日期:2004.2.1
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.