Department of Medicine III, Klinikum Rechts der Isar, Technical University of Munich, Munich, Germany.
TranslaTUM, Center for Translational Cancer Research, Technical University of Munich, Munich, Germany.
EMBO J. 2022 Oct 17;41(20):e110871. doi: 10.15252/embj.2022110871. Epub 2022 Sep 5.
Deubiquitylases (DUBs) are therapeutically amenable components of the ubiquitin machinery that stabilize substrate proteins. Their inhibition can destabilize oncoproteins that may otherwise be undruggable. Here, we screened for DUB vulnerabilities in multiple myeloma, an incurable malignancy with dependency on the ubiquitin proteasome system and identified OTUD6B as an oncogene that drives the G1/S-transition. LIN28B, a suppressor of microRNA biogenesis, is specified as a bona fide cell cycle-specific substrate of OTUD6B. Stabilization of LIN28B drives MYC expression at G1/S, which in turn allows for rapid S-phase entry. Silencing OTUD6B or LIN28B inhibits multiple myeloma outgrowth in vivo and high OTUD6B expression evolves in patients that progress to symptomatic multiple myeloma and results in an adverse outcome of the disease. Thus, we link proteolytic ubiquitylation with post-transcriptional regulation and nominate OTUD6B as a potential mediator of the MGUS-multiple myeloma transition, a central regulator of MYC, and an actionable vulnerability in multiple myeloma and other tumors with an activated OTUD6B-LIN28B axis.
去泛素化酶(DUBs)是泛素机器中具有治疗潜力的组成部分,可稳定底物蛋白。它们的抑制作用可以使原本不可成药的癌蛋白失稳。在这里,我们在多发性骨髓瘤中筛选 DUB 易损性,多发性骨髓瘤是一种无法治愈的恶性肿瘤,依赖于泛素蛋白酶体系统,我们确定 OTUD6B 是一种驱动 G1/S 转变的致癌基因。LIN28B 是 microRNA 生物发生的抑制剂,被指定为 OTUD6B 的真正细胞周期特异性底物。LIN28B 的稳定驱动 MYC 在 G1/S 处表达,进而允许快速进入 S 期。沉默 OTUD6B 或 LIN28B 可抑制体内多发性骨髓瘤的生长,在进展为有症状多发性骨髓瘤的患者中 OTUD6B 表达升高,并导致疾病的不良结局。因此,我们将蛋白水解泛素化与转录后调控联系起来,并将 OTUD6B 作为 MGUS-多发性骨髓瘤转化的潜在介质、MYC 的中央调节剂以及在激活的 OTUD6B-LIN28B 轴的多发性骨髓瘤和其他肿瘤中的可操作弱点来提名。