一二三四区视频,亚洲少妇熟女色,日本久热无码视频网,欧美国产日韩大尺度,亚洲a视频,久久少妇一区二区,日韩999无码视频,刺激久久久久久久,啊啊啊啊不要啊在线

ChemicalBook >> journal list >> Analytical biochemistry >>article
Analytical biochemistry

Analytical biochemistry

IF: 2.6
Download PDF

Optimizations of a novel fluorescence polarization-based high-throughput screening assay for β-catenin/LEF1 interaction inhibitors

Published:1 January 2021 DOI: 10.1016/j.ab.2020.113966 PMID: 32956692
Yunyu Chen , Zhenghao Fu , Dongsheng Li , Yuhuan Yue , Xiaoping Liu

Abstract

Aberrant activation of the Wnt/β-catenin signaling pathway is prominent in the development and metastasis of non-small cell lung cancer (NSCLC). Highly effective inhibition of this pathway highlights a therapeutic avenue against NSCLC. Moreover, β-catenin/LEF1 interaction regulates β-catenin nuclear transport as well as the transcriptions of the key oncogenes in Wnt/β-catenin signaling pathway. Therefore, interruption of this interaction would be a promising therapeutic strategy for NSCLC metastasis. To date, no economical and rapid high-throughput screening (HTS) assay has been reported for the discovery of β-catenin/LEF1 interaction inhibitors. In this study, we developed a novel fluorescence polarization (FP)-based HTS assay to identify β-catenin/LEF1 interaction inhibitors. The FITC-LEF1 sequence, incubation time, temperature, and DMSO resistance were optimized, and then a high Z′ factor of 0.77 was achieved. A pilot screening of a natural product library via this established FP screening assay identified sanguinarine analogues as potential β-catenin/LEF1 interaction inhibitors. GST pull-down and surface plasmon resonance (SPR) assay demonstrated that β-catenin/LEF1 interaction is a potential anticancer target of sanguinarine in vitro. This newly developed FP screening assay will be vital for the rapid discovery of novel Wnt inhibitors targeting β-catenin/LEF1 interaction.

Substances (6)

Materials
Procduct Name CAS Molecular Formula Supplier Price
SANGUINARINE 2447-54-3 C20H14NO4 279 suppliers $45.00-$1850.00
SANGUINARINE 2447-54-3 C20H14NO4 279 suppliers $45.00-$1850.00
SANGUINARINE 2447-54-3 C20H14NO4 279 suppliers $45.00-$1850.00
SANGUINARINE 2447-54-3 C20H14NO4 279 suppliers $45.00-$1850.00
Sanguinarine 2447-54-3 - Inquiry
Sanguinarine 2447-54-3 - Inquiry
平乡县| 博乐市| 武威市| 铜鼓县| 阜宁县| 湟源县| 清丰县| 玉屏| 启东市| 稻城县| 申扎县| 定襄县| 通化县| 拜泉县| 安义县| 石门县| 南汇区| 天镇县| 靖州| 页游| 博湖县| 柘城县| 咸丰县| 寻乌县| 天津市| 大关县| 政和县| 西和县| 蚌埠市| 乌什县| 瓦房店市| 平度市| 五峰| 巨野县| 芦山县| 高阳县| 沂源县| 梧州市| 大关县| 白河县| 民乐县|