Department of Surgery, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA.
Department of Chemical Biology and Therapeutics, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA.
STAR Protoc. 2021 Aug 26;2(3):100702. doi: 10.1016/j.xpro.2021.100702. eCollection 2021 Sep 17.
Identification of diverse chemotypes of selective KDM4 inhibitors is important for exploring and validating the roles of KDM4s in the pathogenesis of human disease and for developing therapies. Here, we report a protocol for high-throughput screening of KDM4 inhibitors using TR-FRET demethylation functional assay. We describe this protocol for screen of KDM4B inhibitors, which can be modified to screen inhibitors of other JmjC-domain-containing KDMs. For complete details on the use and execution of this protocol, please refer to Singh et al. (2021).
鉴定选择性 KDM4 抑制剂的多种化学型对于探索和验证 KDM4 在人类疾病发病机制中的作用以及开发治疗方法非常重要。 在这里，我们报告了一种使用 TR-FRET 去甲基化功能测定法进行高通量筛选 KDM4 抑制剂的方案。 我们描述了这种筛选 KDM4B 抑制剂的方案，该方案可以修改以筛选其他包含 JmjC 结构域的 KDM 的抑制剂。 有关此方案的使用和执行的完整详细信息，请参阅 Singh 等人。 （2021 年）。
