National "111" Center for Cellular Regulation and Molecular Pharmaceutics, Hubei University of Technology, Wuhan, China; Department of Biological Engineering and Key Laboratory of Industrial Fermentation (Ministry of Education), Hubei University of Technology, Wuhan, China.
National "111" Center for Cellular Regulation and Molecular Pharmaceutics, Hubei University of Technology, Wuhan, China; Department of Biological Engineering and Key Laboratory of Industrial Fermentation (Ministry of Education), Hubei University of Technology, Wuhan, China.
Biophys J. 2019 Oct 1;117(7):1301-1310. doi: 10.1016/j.bpj.2019.08.026. Epub 2019 Aug 29.
CREB-binding protein is a multidomain transcriptional coactivator whose transcriptional adaptor zinc-binding 1 (TAZ1) domain mediates interactions with a number of intrinsically disordered transactivation domains (TADs), including the CREB-binding protein/p300-interacting transactivator with ED-rich tail, the hypoxia inducible factor 1α, p53, the signal transducer and activator of transcription 2, and the NF-κB p65 subunit. These five disordered TADs undergo partial disorder-to-order transitions upon binding TAZ1, forming fuzzy complexes with helical segments. Interestingly, they wrap around TAZ1 with different orientations and occupy the binding sites with various orders. To elucidate the microscopic molecular details of the binding processes of TADs with TAZ1, in this work, we carried out extensive molecular dynamics simulations using a coarse-grained topology-based model. After careful calibration of the models to reproduce the residual helical contents and binding affinities, our simulations were able to recapitulate the experimentally observed flexibility profiles. Although great differences exist in the complex structures, we found similarities between hypoxia inducible factor 1α and signal transducer and activator of transcription 2 as well as between CREB-binding protein/p300-interacting transactivator with ED-rich tail and NF-κB p65 subunit in the binding kinetics and binding thermodynamics. Although the origins of similarities and differences in the binding mechanisms remain unclear, our results provide some clues that indicate that binding of TADs to TAZ1 could be templated by the target as well as encoded by the TADs.
CREB 结合蛋白是一种多功能转录共激活因子,其转录适配器锌结合 1(TAZ1)结构域介导与许多固有无序的转录激活结构域(TAD)的相互作用,包括 CREB 结合蛋白/ p300 相互作用的转录激活因子具有 ED 丰富的尾巴、缺氧诱导因子 1α、p53、信号转导和转录激活因子 2、以及 NF-κB p65 亚基。这五个无序 TAD 在与 TAZ1 结合时会发生部分无序到有序的转变,形成带有螺旋片段的模糊复合物。有趣的是,它们以不同的方向围绕 TAZ1 缠绕,并以不同的顺序占据结合位点。为了阐明 TAD 与 TAZ1 结合过程的微观分子细节,在这项工作中,我们使用基于粗粒度拓扑的模型进行了广泛的分子动力学模拟。在仔细校准模型以重现剩余的螺旋含量和结合亲和力之后,我们的模拟能够再现实验观察到的灵活性分布。尽管复合物结构存在很大差异,但我们发现缺氧诱导因子 1α和信号转导和转录激活因子 2 之间以及 CREB 结合蛋白/ p300 相互作用的转录激活因子具有 ED 丰富的尾巴和 NF-κB p65 亚基之间存在相似性在结合动力学和结合热力学方面。尽管结合机制中的相似性和差异性的起源尚不清楚,但我们的结果提供了一些线索,表明 TAD 与 TAZ1 的结合可能受到靶标的模板作用以及 TAD 编码的影响。