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β-连环蛋白介导的信号通路新型小分子激活剂:靛玉红的构效关系

Novel small molecule activators of beta-catenin-mediated signaling pathway: structure-activity relationships of indirubins.

作者信息

Park Eun-Jung, Choi Soo Jeong, Kim Yong-Chul, Lee Sang Hyung, Park Seoung Woo, Lee Sang Kook

机构信息

College of Pharmacy, Ewha Womans University, Seoul, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2282-4. doi: 10.1016/j.bmcl.2009.02.083. Epub 2009 Feb 26.

DOI:10.1016/j.bmcl.2009.02.083
PMID:19282173
Abstract

Based on the beta-catenin-drived Wnt activator of bromoindirubin-3'-oxime (BIO), indirubin analogs were evaluated for beta-catenin-mediated gene expression. A novel indirubin analog, indirubin-5-nitro-3'-oxime (INO), was considered a potential activator, and structure-activity studies were conducted with indirubins. These data suggest that INO might be a novel Wnt activator and has a potential of signaling regulator in beta-catenin-mediated signaling pathways.

摘要

基于溴靛玉红-3'-肟(BIO)的β-连环蛋白驱动的Wnt激活剂,对靛玉红类似物进行了β-连环蛋白介导的基因表达评估。一种新型靛玉红类似物,靛玉红-5-硝基-3'-肟(INO),被认为是一种潜在的激活剂,并对靛玉红进行了构效关系研究。这些数据表明,INO可能是一种新型Wnt激活剂,在β-连环蛋白介导的信号通路中具有信号调节剂的潜力。

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