Institute for Modeling Collaboration and Innovation, University of Idaho, Moscow 83844, Idaho, United States.
Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine and Children's Healthcare of Atlanta, Atlanta 30322, Georgia, United States.
J Chem Inf Model. 2022 Mar 14;62(5):1282-1293. doi: 10.1021/acs.jcim.1c01104. Epub 2022 Feb 23.
Serum albumin is the most abundant protein in blood plasma, and it is involved in multiple biological processes. Serum albumin has recently been adapted for improving biomaterial integration with bone tissue, and studies have shown the importance of this protein in bone repair and regeneration. However, the mechanism of action is not yet clear. In stark contrast, other studies have demonstrated that albumin blocks cell adhesion to surfaces, which is seen as a limitation to its bone healing role. These apparent contradictions suggest that the conformation of albumin facilitates its bioactivity, leading to enhanced bone repair. Serum albumin is known to play a major role in maintaining the calcium ion concentration in blood plasma. Due to the prevalence of calcium at bone repair and regeneration sites, it has been hypothesized that calcium binding to serum albumin triggers a conformational change, leading to bioactivity. In the current study, molecular modeling approaches including molecular docking, atomic molecular dynamics (MD) simulation, and coarse-grained MD simulation were used to test this hypothesis by investigating the conformational changes induced in bovine serum albumin by interaction with calcium ions. The computational results were qualitatively validated with experimental Fourier-transform infrared spectroscopy analysis. We find that free calcium ions in solution transiently bind with the three major loops in albumin, triggering a conformational change where N-terminal and C-terminal domains separate from each other in a partial unfolding process. The separation distance between these domains was found to correlate with the calcium ion concentration. The experimental data support the simulation results showing that albumin has enhanced conformational heterogeneity upon exposure to intermediate levels of calcium, without any significant secondary structure changes.
血清白蛋白是血浆中最丰富的蛋白质,参与多种生物学过程。最近,血清白蛋白被用于改善生物材料与骨组织的整合,研究表明这种蛋白质在骨修复和再生中非常重要。然而,其作用机制尚不清楚。与此形成鲜明对比的是,其他研究表明白蛋白会阻止细胞黏附在表面上,这被认为是其在骨愈合中的作用的一个限制。这些明显的矛盾表明,白蛋白的构象促进了其生物活性,从而增强了骨修复。血清白蛋白在维持血浆中钙离子浓度方面起着重要作用。由于钙在骨修复和再生部位的普遍存在,有人假设钙与血清白蛋白结合会引发构象变化,从而产生生物活性。在当前的研究中,使用分子对接、原子分子动力学(MD)模拟和粗粒 MD 模拟等分子建模方法,通过研究钙离子与牛血清白蛋白相互作用所引起的构象变化,来验证这一假设。计算结果通过傅里叶变换红外光谱分析的实验定性验证。我们发现,溶液中的游离钙离子会与白蛋白的三个主要环短暂结合,触发构象变化,导致 N 端和 C 端结构域在部分展开过程中彼此分离。发现这些结构域之间的分离距离与钙离子浓度相关。实验数据支持模拟结果表明,白蛋白在暴露于中等水平的钙离子时具有增强的构象异质性,而没有明显的二级结构变化。