一种 6 聚体光控寡核苷酸作为有效的端粒酶抑制剂。

A 6-mer photocontrolled oligonucleotide as an effective telomerase inhibitor.

机构信息

Research Center for Advanced Science and Technology, The University of Tokyo, 4-6-1 Komaba, Meguro-ku, Tokyo 153-8904, Japan.

出版信息

J Am Chem Soc. 2010 Jan 20;132(2):631-7. doi: 10.1021/ja907417r.

DOI:10.1021/ja907417r

PMID:20014834

Abstract

Telomerase is a relevant target for cancer therapy. A small 6-mer psoralen-containing oligonucleotide is shown to cause efficient photo-cross-linking to human telomere DNA by G-quadruplex formation. The small, photocontrolled oligonucleotide shows effective telomerase inhibition, both in vitro and in vivo, only when light irradiated. Data suggest that it is a promising agent for the treatment of cancer.

摘要

端粒酶是癌症治疗的一个相关靶点。研究表明，一种含有 6 个碱基的小 psoralen 寡核苷酸通过 G-四链体的形成导致人端粒 DNA 的有效光交联。这种小的、光控的寡核苷酸在体外和体内都显示出有效的端粒酶抑制作用，只有在光照下才会发生。数据表明，它是一种有前途的癌症治疗药物。