Discovery of novel trimethoxy-ring BRD4 bromodomain inhibitors: AlphaScreen assay, crystallography and cell-based assay

As a member of the bromodomain and extra terminal domain (BET) protein family, BRD4 is closely related to cancers and other diseases. Small-molecule BRD4 inhibitors have already demonstrated promising potential for the therapy of BRD4-related cancers. In this study, we report the discovery and evalu...

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Bibliographic Details
Published in:Medchemcomm
Main Authors: Chen, Zhifeng, Zhang, Hao, Liu, Shien, Xie, Yiqian, Jiang, Hao, Lu, Wenchao, Xu, Heng, Yue, Liyan, Zhang, Yuanyuan, Ding, Hong, Zheng, Mingyue, Yu, Kunqian, Chen, Kaixian, Jiang, Hualiang, Luo, Cheng
Format: Artigo
Language:Inglês
Published: Royal Society of Chemistry 2017
Subjects:
Chemistry
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6071828/
https://ncbi.nlm.nih.gov/pubmed/30108844
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c7md00083a
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