DNA结合型吡咯-咪唑聚酰胺的快速固相合成

Rapid solid-phase synthesis of DNA-binding pyrrole-imidazole polyamides.

作者信息

Krutzik Peter O, Chamberlin A Richard

机构信息

Department of Chemistry, University of California-Irvine, CA 92697, Irvine, USA.

出版信息

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2129-32. doi: 10.1016/s0960-894x(02)00359-1.

DOI:10.1016/s0960-894x(02)00359-1

PMID:12127520

Abstract

Pyrrole-imidazole polyamides can be synthesized to target predetermined sequences of DNA with nanomolar affinity and high specificity, and have been shown to modulate gene transcription both in vitro and in vivo. To make polyamides more readily available to biological laboratories, we have developed a rapid solid-phase synthesis based on azabenzotriazole (OAt) activation that decreases synthesis time 60% compared to standard benzotriazole (OBt) techniques, without loss of yield or purity.

摘要

吡咯-咪唑聚酰胺能够被合成以靶向具有纳摩尔亲和力和高特异性的预定DNA序列，并且已证实在体外和体内均可调节基因转录。为了使生物实验室更易于获得聚酰胺，我们开发了一种基于氮杂苯并三唑（OAt）活化的快速固相合成方法，与标准苯并三唑（OBt）技术相比，该方法可将合成时间缩短60%，且不会损失产率或纯度。