Cao Shiyun, Shi Huigang, Garcia Sheena Faye, Kito Yuki, Shi Hui, Goldberg Hailey V, Ponce Jackeline, Ueberheide Beatrix, Lignitto Luca, Pagano Michele, Zheng Ning
Department of Pharmacology, Box 357280, University of Washington, Seattle, WA, USA.
Howard Hughes Medical Institute, University of Washington, Seattle, WA, USA.
bioRxiv. 2024 Jun 3:2024.06.03.594717. doi: 10.1101/2024.06.03.594717.
The transcription factor BACH1 regulates heme homeostasis and oxidative stress responses and promotes cancer metastasis upon aberrant accumulation. Its stability is controlled by two F-box protein ubiquitin ligases, FBXO22 and FBXL17. Here we show that the homodimeric BTB domain of BACH1 functions as a previously undescribed quaternary structure degron, which is deciphered by the two F-box proteins via distinct mechanisms. After BACH1 is released from chromatin by heme, FBXO22 asymmetrically recognizes a cross-protomer interface of the intact BACH1 BTB dimer, which is otherwise masked by the co-repressor NCOR1. If the BACH1 BTB dimer escapes the surveillance by FBXO22 due to oxidative modifications, its quaternary structure integrity is probed by a pair of FBXL17, which simultaneously engage and remodel the two BTB protomers into E3-bound monomers for ubiquitination. By unveiling the multifaceted regulatory mechanisms of BACH1 stability, our studies highlight the abilities of ubiquitin ligases to decode high-order protein assemblies and reveal therapeutic opportunities to block cancer invasion via compound-induced BACH1 destabilization.
转录因子BACH1调节血红素稳态和氧化应激反应,并在异常积累时促进癌症转移。其稳定性由两种F-box蛋白泛素连接酶FBXO22和FBXL17控制。在此我们表明,BACH1的同二聚体BTB结构域作为一种前所未有的四级结构降解子发挥作用,这两种F-box蛋白通过不同机制对其进行识别。血红素使BACH1从染色质上释放后,FBXO22不对称地识别完整的BACH1 BTB二聚体的跨原体界面,该界面在其他情况下被共抑制因子NCOR1掩盖。如果BACH1 BTB二聚体由于氧化修饰而逃脱了FBXO22的监测,其四级结构完整性会被一对FBXL17检测,FBXL17会同时结合并将两个BTB原体重塑为与E3结合的单体以进行泛素化。通过揭示BACH1稳定性的多方面调控机制,我们的研究突出了泛素连接酶解码高阶蛋白质组装体的能力,并揭示了通过化合物诱导BACH1不稳定来阻断癌症侵袭的治疗机会。