MNK2 缺乏通过翻译调控增强β细胞再生。
MNK2 deficiency potentiates β-cell regeneration via translational regulation.
机构信息
Department of Cell and Molecular Biology, Karolinska Institutet, Stockholm, Sweden.
Science for Life Laboratory, Department of Oncology-Pathology, Karolinska Institutet, Solna, Sweden.
出版信息
Nat Chem Biol. 2022 Sep;18(9):942-953. doi: 10.1038/s41589-022-01047-x. Epub 2022 Jun 13.
Regenerating pancreatic β-cells is a potential curative approach for diabetes. We previously identified the small molecule CID661578 as a potent inducer of β-cell regeneration, but its target and mechanism of action have remained unknown. We now screened 257 million yeast clones and determined that CID661578 targets MAP kinase-interacting serine/threonine kinase 2 (MNK2), an interaction we genetically validated in vivo. CID661578 increased β-cell neogenesis from ductal cells in zebrafish, neonatal pig islet aggregates and human pancreatic ductal organoids. Mechanistically, we found that CID661578 boosts protein synthesis and regeneration by blocking MNK2 from binding eIF4G in the translation initiation complex at the mRNA cap. Unexpectedly, this blocking activity augmented eIF4E phosphorylation depending on MNK1 and bolstered the interaction between eIF4E and eIF4G, which is necessary for both hypertranslation and β-cell regeneration. Taken together, our findings demonstrate a targetable role of MNK2-controlled translation in β-cell regeneration, a role that warrants further investigation in diabetes.
再生胰腺β细胞是糖尿病的一种有潜力的治疗方法。我们之前发现小分子 CID661578 是一种有效的β细胞再生诱导剂,但它的靶点和作用机制仍不清楚。我们现在筛选了 2.57 亿个酵母克隆,并确定 CID661578 的靶点是丝氨酸/苏氨酸激酶 2(MNK2),我们在体内遗传验证了这种相互作用。CID661578 可促进斑马鱼、新生猪胰岛聚集物和人胰腺导管类器官中的导管细胞向β细胞新生。从机制上讲,我们发现 CID661578 通过阻止 MNK2 在翻译起始复合物中与 mRNA 帽结合,从而阻止 MNK2 与 eIF4G 结合,从而增强蛋白质合成和再生。出乎意料的是,这种阻断活性增强了 eIF4E 的磷酸化,这取决于 MNK1,并增强了 eIF4E 和 eIF4G 之间的相互作用,这对于超翻译和β细胞再生都是必需的。综上所述,我们的研究结果表明 MNK2 控制的翻译在β细胞再生中起着可靶向的作用,这一作用值得在糖尿病中进一步研究。
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