Department of Molecular and Cell Biology, University of California, Berkeley, CA 94720.
Proc Natl Acad Sci U S A. 2014 Jan 7;111(1):237-42. doi: 10.1073/pnas.1302823110. Epub 2013 Dec 20.
To increase the power of X-ray crystallography to determine not only the structures but also the motions of biomolecules, we developed methods to address two classic crystallographic problems: putting electron density maps on the absolute scale of e(-)/Å(3) and calculating the noise at every point in the map. We find that noise varies with position and is often six to eight times lower than thresholds currently used in model building. Analyzing the rescaled electron density maps from 485 representative proteins revealed unmodeled conformations above the estimated noise for 45% of side chains and a previously hidden, low-occupancy inhibitor of HIV capsid protein. Comparing the electron density maps in the free and nucleotide-bound structures of three human protein kinases suggested that substrate binding perturbs distinct intrinsic allosteric networks that link the active site to surfaces that recognize regulatory proteins. These results illustrate general approaches to identify and analyze alternative conformations, low-occupancy small molecules, solvent distributions, communication pathways, and protein motions.
为了提高 X 射线晶体学的能力,不仅确定生物分子的结构,而且确定其运动,我们开发了一些方法来解决两个经典的晶体学问题:将电子密度图置于电子/埃(3)的绝对标度上,并计算图谱中每个点的噪声。我们发现噪声随位置而变化,并且通常比当前用于模型构建的阈值低六到八倍。对来自 485 个代表性蛋白质的重新标度电子密度图进行分析,发现 45%的侧链存在未建模的构象,高于估计的噪声,此外还有一种先前隐藏的 HIV 衣壳蛋白的低占据抑制剂。比较三种人类蛋白激酶的游离和核苷酸结合结构中的电子密度图表明,底物结合会扰乱将活性位点与识别调节蛋白的表面连接起来的不同内在变构网络。这些结果说明了识别和分析替代构象、低占据小分子、溶剂分布、通讯途径和蛋白质运动的一般方法。