Notch 抑制剂筛选揭示了一种意想不到的 HES1 异二聚体。
Notch inhibitor screening reveals an unexpected HES1 heterodimer.
机构信息
Department of Medicine, Cedars-Sinai Medical Center, Los Angeles, California 90048.
Department of Medicine, Cedars-Sinai Medical Center, Los Angeles, California 90048; Department of Research, Greater Los Angeles Veterans Affairs Hospital, Los Angeles, California 90048.
出版信息
J Biol Chem. 2018 May 25;293(21):8295-8296. doi: 10.1074/jbc.H118.002880.
Abstract
Notch signaling plays critical roles in cancer progression, motivating efforts to identify inhibitors of this pathway. Perron report a small-molecule screen intended to discover compounds that could interfere with the downstream transcription factor HES1. Target validation of their compounds unexpectedly identified a novel HES1-interacting protein, prohibitin 2. This highlights a new mechanism to block Notch signaling and prompting further exploration of HES1 biology.
摘要
Notch 信号通路在癌症进展中起着关键作用，这促使人们努力寻找该途径的抑制剂。Perron 等人报告了一项旨在发现可能干扰下游转录因子 HES1 的化合物的小分子筛选。他们的化合物的靶标验证出人意料地鉴定出一种新型的 HES1 相互作用蛋白，即 prohibitin 2。这突出了阻断 Notch 信号的新机制，并促使进一步探索 HES1 的生物学。
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