表型筛选
计算生物学
表型
药物发现
生物标志物
生物
仿形(计算机编程)
癌症
蛋白质组学
生物标志物发现
蛋白质组
癌细胞
小分子
癌症研究
生物信息学
遗传学
生物化学
基因
计算机科学
操作系统
作者
Ke Cheng,Jung Hoon Lee,Piliang Hao,Shao Q. Yao,Ke Ding,Zhengqiu Li
标识
DOI:10.1002/anie.201709584
摘要
Target-identification phenotypic screening has been a powerful approach in drug discovery; however, it is hindered by difficulties in identifying the underlying cellular targets. To address this challenge, we have combined phenotypic screening of a fully functionalized small-molecule library with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits. Using this approach, we identified ANXA2, PDIA3/4, FLAD1, and NOS2 as primary cellular targets of two bioactive molecules that inhibit cancer cell proliferation. We further demonstrated that a panel of probes can label and/or image annexin A2 (a cancer biomarker) from different cancer cell lines, thus providing opportunities for potential cancer diagnosis and therapy.
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