Department of Chemistry, The Pennsylvania State University, University Park, Pennsylvania, USA.
Protein Sci. 2021 Mar;30(3):543-557. doi: 10.1002/pro.4011. Epub 2020 Dec 19.
Experimental observations of enzymes under active turnover conditions have brought new insight into the role of protein motions and allosteric networks in catalysis. Many of these studies characterize enzymes under dynamic chemical equilibrium conditions, in which the enzyme is actively catalyzing both the forward and reverse reactions during data acquisition. We have previously analyzed conformational dynamics and allosteric networks of the alpha subunit of tryptophan synthase under such conditions using NMR. We have proposed that this working state represents a four to one ratio of the enzyme bound with the indole-3-glycerol phosphate substrate (E:IGP) to the enzyme bound with the products indole and glyceraldehyde-3-phosphate (E:indole:G3P). Here, we analyze the inactive D60N variant to deconvolute the contributions of the substrate- and products-bound states to the working state. While the D60N substitution itself induces small structural and dynamic changes, the D60N E:IGP and E:indole:G3P states cannot entirely account for the conformational dynamics and allosteric networks present in the working state. The act of chemical bond breakage and/or formation, or possibly the generation of an intermediate, may alter the structure and dynamics present in the working state. As the enzyme transitions from the substrate-bound to the products-bound state, millisecond conformational exchange processes are quenched and new allosteric connections are made between the alpha active site and the surface which interfaces with the beta subunit. The structural ordering of the enzyme and these new allosteric connections may be important in coordinating the channeling of the indole product into the beta subunit.
在活跃的周转条件下对酶进行的实验观察为蛋白质运动和变构网络在催化中的作用带来了新的认识。这些研究中的许多都是在动态化学平衡条件下对酶进行研究的,在这种条件下,酶在数据采集过程中积极地催化正向和反向反应。我们以前使用 NMR 分析了色氨酸合酶α亚基在这种条件下的构象动力学和变构网络。我们提出,这种工作状态代表了与吲哚-3-甘油磷酸底物(E:IGP)结合的酶与与产物吲哚和甘油醛-3-磷酸(E:吲哚:G3P)结合的酶的四比一的比例。在这里,我们分析了不活跃的 D60N 变体,以剖析底物和产物结合状态对工作状态的贡献。虽然 D60N 取代本身会引起微小的结构和动力学变化,但 D60N E:IGP 和 E:吲哚:G3P 状态不能完全解释工作状态中存在的构象动力学和变构网络。化学键的断裂和/或形成的作用,或者可能是中间产物的产生,可能会改变工作状态中存在的结构和动力学。当酶从底物结合状态转变为产物结合状态时,毫秒级别的构象交换过程被猝灭,并且在α活性位点和与β亚基接口的表面之间建立了新的变构连接。酶的结构有序性和这些新的变构连接可能对于协调吲哚产物进入β亚基的通道化很重要。