Discovery of novel aromatase inhibitors using a homogeneous time-resolved fluorescence assay

@inproceedings{Ji2014DiscoveryON,
  title={Discovery of novel aromatase inhibitors using a homogeneous time-resolved fluorescence assay},
  author={Jin-zi Ji and Ke-jing Lao and Jie Hu and Tao Pang and Zhen-zhou Jiang and Hao-liang Yuan and Jing-shan Miao and Xin Chen and Shan-shan Ning and Hua Xiang and Yu-meng Guo and Ming Yan and Lu-yong Zhang},
  booktitle={Acta Pharmacologica Sinica},
  year={2014}
}
Aim:Aromatase is an important target for drugs to treat hormone-dependent diseases, including breast cancer. The aim of this study was to develop a homogeneous time-resolved fluorescence (HTRF) aromatase assay suitable for high-throughput screening (HTS).Methods:A 384-well aromatase HTRF assay was established, and used to screen about 7000 compounds from a compound library. Anti-proliferation activity of the hit was evaluated using alamarBlue(R) assay in a hormone-dependent breast cancer cell… CONTINUE READING