Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins
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https://figshare.com/articles/dataset/Exploring_Selective_Inhibition_of_the_First_Bromodomain_of_the_Human_Bromodomain_and_Extra_terminal_Domain_BET_Proteins/2091187
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资源简介：
A midthroughput
screening follow-up program targeting the first
bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic
xanthine derivative inhibitor. This compound binds with an affinity
in the low micromolar range yet exerts suitable unexpected selectivity in vitro against the other members of the bromodomain and
extra-terminal domain (BET) family. A structure-based program pinpointed
a role of the ZA loop, paving the way for the development of potent
and selective BET-BRDi probes.
创建时间：
2016-02-19
