Aurora B 激酶多步别构激活的结构基础。

The structural basis of the multi-step allosteric activation of Aurora B kinase.

机构信息

Centre for Molecular Medicine Norway (NCMM), Nordic EMBL Partnership, Faculty of Medicine, Oslo, Norway.

Department of Biosciences, University of Oslo, Oslo, Norway.

出版信息

Elife. 2023 May 25;12:e85328. doi: 10.7554/eLife.85328.

Abstract

Aurora B, together with IN-box, the C-terminal part of INCENP, forms an enzymatic complex that ensures faithful cell division. The [Aurora B/IN-box] complex is activated by autophosphorylation in the Aurora B activation loop and in IN-box, but it is not clear how these phosphorylations activate the enzyme. We used a combination of experimental and computational studies to investigate the effects of phosphorylation on the molecular dynamics and structure of [Aurora B/IN-box]. In addition, we generated partially phosphorylated intermediates to analyze the contribution of each phosphorylation independently. We found that the dynamics of Aurora and IN-box are interconnected, and IN-box plays both positive and negative regulatory roles depending on the phosphorylation status of the enzyme complex. Phosphorylation in the activation loop of Aurora B occurs intramolecularly and prepares the enzyme complex for activation, but two phosphorylated sites are synergistically responsible for full enzyme activity.

摘要

极光 B 与盒内,INCENP 的 C 末端部分,形成一个酶复合物,确保忠实的细胞分裂。[极光 B/盒内]复合物通过在极光 B 激活环和盒内的自身磷酸化激活,但目前尚不清楚这些磷酸化如何激活酶。我们使用实验和计算研究的组合来研究磷酸化对[极光 B/盒内]的分子动力学和结构的影响。此外,我们生成了部分磷酸化的中间产物,以独立分析每个磷酸化的贡献。我们发现极光和盒内的动力学是相互关联的,盒内根据酶复合物的磷酸化状态发挥正、负调节作用。极光 B 的激活环中的磷酸化发生在分子内,为酶复合物的激活做准备,但两个磷酸化位点协同负责完全的酶活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee09/10259393/5616b55519fe/elife-85328-fig1.jpg

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