Leumann Christian J
Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, CH-3012, Bern, Switzerland.
Bioorg Med Chem. 2002 Apr;10(4):841-54. doi: 10.1016/s0968-0896(01)00348-0.
Mainly driven by the needs of antisense research, a large number of oligonucleotide analogues have been prepared and evaluated over the last 15 years. Besides minor structural modifications of the building blocks of DNA and RNA itself, a considerable effort has been devoted to the de novo design of nucleoside analogues with improved binding properties. A particularly successful concept turned out to be that of conformational restriction. This review focuses on recent advances in this area and tries to summarize scope and limitations of this design principle.
在过去15年里，主要受反义研究需求的驱动，人们制备并评估了大量的寡核苷酸类似物。除了对DNA和RNA自身的组成单元进行微小的结构修饰外，人们还投入了大量精力进行具有更好结合特性的核苷类似物的从头设计。结果发现，一个特别成功的概念是构象限制。本综述聚焦于该领域的最新进展，并试图总结这一设计原则的适用范围和局限性。
