Department of Translational Research in Psychiatry, Max Planck Institute of Psychiatry, Kraepelinstr. 10, 80804, Munich, Germany.
Department of Psychiatry and Psychotherapy, University of Bonn, Venusberg Campus 1, 53127, Bonn, Germany.
Nat Commun. 2019 Dec 18;10(1):5770. doi: 10.1038/s41467-019-13659-4.
Autophagy is an essential cellular process affecting virus infections and other diseases and Beclin1 (BECN1) is one of its key regulators. Here, we identified S-phase kinase-associated protein 2 (SKP2) as E3 ligase that executes lysine-48-linked poly-ubiquitination of BECN1, thus promoting its proteasomal degradation. SKP2 activity is regulated by phosphorylation in a hetero-complex involving FKBP51, PHLPP, AKT1, and BECN1. Genetic or pharmacological inhibition of SKP2 decreases BECN1 ubiquitination, decreases BECN1 degradation and enhances autophagic flux. Middle East respiratory syndrome coronavirus (MERS-CoV) multiplication results in reduced BECN1 levels and blocks the fusion of autophagosomes and lysosomes. Inhibitors of SKP2 not only enhance autophagy but also reduce the replication of MERS-CoV up to 28,000-fold. The SKP2-BECN1 link constitutes a promising target for host-directed antiviral drugs and possibly other autophagy-sensitive conditions.
自噬是影响病毒感染和其他疾病的一种基本的细胞过程,Beclin1(BECN1)是其关键调节因子之一。在这里,我们鉴定出 S 期激酶相关蛋白 2(SKP2)作为 E3 连接酶,对 BECN1 执行赖氨酸 48 位连接的多泛素化,从而促进其蛋白酶体降解。SKP2 的活性通过 FKBP51、PHLPP、AKT1 和 BECN1 异源复合物中的磷酸化调节。SKP2 的遗传或药理学抑制降低了 BECN1 的泛素化,降低了 BECN1 的降解并增强了自噬流。中东呼吸综合征冠状病毒(MERS-CoV)的增殖导致 BECN1 水平降低,并阻断自噬体和溶酶体的融合。SKP2 的抑制剂不仅增强了自噬,而且将 MERS-CoV 的复制减少了 28,000 倍。SKP2-BECN1 联系构成了针对宿主定向抗病毒药物的有前途的靶标,并且可能还有其他自噬敏感的情况。