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一种用于肽核酸的环戊烷构象限制:设计、不对称合成以及对DNA和RNA的结合亲和力提高

A cyclopentane conformational restraint for a peptide nucleic acid: design, asymmetric synthesis, and improved binding affinity to DNA and RNA.

作者信息

Myers Michael C, Witschi Mark A, Larionova Nataliya V, Franck John M, Haynes Russell D, Hara Toshiaki, Grajkowski Andrzej, Appella Daniel H

机构信息

Department of Chemistry, Northwestern University, Evanston, Illinois 60208, USA.

出版信息

Org Lett. 2003 Jul 24;5(15):2695-8. doi: 10.1021/ol0348811.

DOI:10.1021/ol0348811
PMID:12868892
Abstract

[structure: see text] A strategy to restrict the highly flexible backbone conformation of a peptide nucleic acid (PNA) by incorporation of a cyclopentane ring is proposed. An asymmetric synthesis of cyclopentane-modified PNA is reported, and its binding properties were determined. The cyclopentane ring leads to a significant improvement in the binding properties of the resulting PNA to DNA and RNA.

摘要

[结构:见正文] 提出了一种通过并入环戊烷环来限制肽核酸(PNA)高度灵活的主链构象的策略。报道了环戊烷修饰的PNA的不对称合成,并测定了其结合特性。环戊烷环使所得PNA与DNA和RNA的结合特性有显著改善。

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