Laboratory for Conservation and Utilization of Bio-Resources, Yunnan University, Kunming, Yunnan, People's Republic of China.
J Mol Model. 2011 Feb;17(2):289-300. doi: 10.1007/s00894-010-0724-6. Epub 2010 May 6.
The native serine protease proteinase K binds two calcium cations. It has been reported that Ca(2+) removal decreased the enzyme's thermal stability and to some extent the substrate affinity, but has discrepant effects on catalytic activity of the enzyme. Molecular dynamics simulations were performed on the Ca(2+)-bound and Ca(2+)-free proteases to investigate the mechanism by which the calciums affect the structural stability, molecular motions, and catalytic activity of proteinase K. Very similar structural properties were observed between these two forms of proteinase K during simulations; and several long-lived hydrogen bonds and salt bridges common to both forms of proteinase K were found to be crucial in maintaining the local conformations around these two Ca(2+) sites. Although Ca(2+) removal enhanced the overall flexibility of proteinase K, the flexibility in a limited number of segments surrounding the substrate-binding pockets decreased. The largest differences in the equilibrium structures of the two simulations indicate that, upon the removal of Ca(2+), the large concerted motion originating from the Ca1 site can transmit to the substrate-binding regions but not to the catalytic triad residues. In conjunction with the large overlap of the essential subspaces between the two simulations, these results not only provide insight into the dynamics of the underlying molecular mechanism responsible for the unchanged enzymatic activity as well as the decreased thermal stability and substrate affinity of proteinase K upon Ca(2+) removal, but also complement the experimentally determined structural and biochemical data.
天然丝氨酸蛋白酶蛋白酶 K 结合两个钙离子。据报道,Ca(2+)的去除降低了酶的热稳定性,并在一定程度上降低了底物亲和力,但对酶的催化活性有不同的影响。对结合 Ca(2+)和无 Ca(2+)的蛋白酶进行分子动力学模拟,以研究 Ca(2+)如何影响蛋白酶 K 的结构稳定性、分子运动和催化活性。在模拟过程中,这两种形式的蛋白酶 K 具有非常相似的结构特性;并且发现两种形式的蛋白酶 K 中存在几个长寿命氢键和盐桥,对于维持这两个 Ca(2+)位点周围的局部构象至关重要。虽然 Ca(2+)的去除增强了蛋白酶 K 的整体灵活性,但围绕底物结合口袋的少数几个片段的灵活性降低了。两种模拟的平衡结构的最大差异表明,在 Ca(2+)去除后,源自 Ca1 位点的大协同运动可以传递到底物结合区域,但不能传递到催化三联体残基。结合两个模拟之间的重要子空间的大量重叠,这些结果不仅提供了对潜在分子机制动力学的深入了解,该机制负责在 Ca(2+)去除时保持酶活性不变以及降低蛋白酶 K 的热稳定性和底物亲和力,而且还补充了实验确定的结构和生化数据。