Process Development, Amgen Inc., 360 Binney St, Cambridge, MA, 02141, USA.
Sci Rep. 2023 Mar 23;13(1):4791. doi: 10.1038/s41598-023-32067-9.
We have investigated the dynamics of two [Formula: see text]-immunoglobulin molecules, IgG1 and IgG4, using long all atom molecular dynamics simulations. We first show that the de novo structures of IgG1 and IgG4 predicted using AlphaFold, with no interactions between the fragment crystallizable (Fc) domain and the antigen fragment binding domain (Fab), eventually relaxes to a state with persistent Fc-Fab interactions that mirrors experimentally resolved structures. We quantified the conformational space sampled by antibody trajectories spawned from six different initial structures and show that the individual trajectories only sample states bound by a local minimum and display very little mixing in their conformational states. Furthermore, the dynamics of the individual Fab domains are strongly dependent on the initial crystal structure and isotype. In all conditions, we observe non-identical dynamics between the Fab arms in an antibody. For a six-bead coarse grained model, we show that non-covalent Fc-Fab interactions can modulate the stiffnesses associated with Fc-Fab distances, angles, and dihedral angles by up to three orders of magnitude. Our results clearly illustrate the inherent complexities in studying antibody dynamics and highlight the need to include non-identical Fab dynamics as an inherent feature in computational models of therapeutic antibodies.
我们使用长全原子分子动力学模拟研究了两种[公式:见正文]免疫球蛋白分子 IgG1 和 IgG4 的动力学。我们首先表明,使用 AlphaFold 预测的 IgG1 和 IgG4 的从头结构,Fc 结构域和抗原片段结合结构域(Fab)之间没有相互作用,最终会松弛到一种具有持久 Fc-Fab 相互作用的状态,这种状态与实验解析结构相吻合。我们量化了由六个不同初始结构产生的抗体轨迹所采样的构象空间,并表明单个轨迹仅采样由局部最小值结合的状态,并且其构象状态几乎没有混合。此外,单个 Fab 结构域的动力学强烈依赖于初始晶体结构和同型。在所有条件下,我们在抗体中观察到 Fab 臂之间的非同源动力学。对于一个六珠粗粒化模型,我们表明非共价 Fc-Fab 相互作用可以通过高达三个数量级来调节与 Fc-Fab 距离、角度和二面角相关的刚度。我们的结果清楚地说明了研究抗体动力学的固有复杂性,并强调需要将非同源 Fab 动力学作为治疗性抗体计算模型的固有特征包含在内。