Department of Chemical Engineering, University of New Hampshire, Durham, New Hampshire, USA.
Proteins. 2023 Jan;91(1):62-73. doi: 10.1002/prot.26410. Epub 2022 Aug 24.
The insulin receptor (IR), the insulin-like growth factor-1 receptor (IGF1R), and the insulin/IGF1 hybrid receptors (hybR) are homologous transmembrane receptors. The peptide ligands, insulin and IGF1, exhibit significant structural homology and can bind to each receptor via site-1 and site-2 residues with distinct affinities. The variants of the Iridoviridae virus family show capability in expressing single-chain insulin/IGF1 like proteins, termed viral insulin-like peptides (VILPs), which can stimulate receptors from the insulin family. The sequences of VILPs lacking the central C-domain (dcVILPs) are known, but their structures in unbound and receptor-bound states have not been resolved to date. We report all-atom structural models of three dcVILPs (dcGIV, dcSGIV, and dcLCDV1) and their complexes with the receptors (μIR, μIGF1R, and μhybR), and probed the peptide/receptor interactions in each system using all-atom molecular dynamics (MD) simulations. Based on the nonbonded interaction energies computed between each residue of peptides (insulin and dcVILPs) and the receptors, we provide details on residues establishing significant interactions. The observed site-1 insulin/μIR interactions are consistent with previous experimental studies, and a residue-level comparison of interactions of peptides (insulin and dcVILPs) with the receptors revealed that, due to sequence differences, dcVILPs also establish some interactions distinct from those between insulin and IR. We also designed insulin analogs and report enhanced interactions between some analogs and the receptors.
胰岛素受体 (IR)、胰岛素样生长因子-1 受体 (IGF1R) 和胰岛素/IGF1 杂合受体 (hybR) 是同源的跨膜受体。肽配体胰岛素和 IGF1 表现出显著的结构同源性,并且可以通过具有不同亲和力的位点 1 和位点 2 残基结合到每个受体上。杆状病毒科病毒家族的变体表现出表达单链胰岛素/IGF1 样蛋白的能力,称为病毒胰岛素样肽 (VILP),其可以刺激胰岛素家族的受体。缺乏中央 C 结构域的 VILP 序列 (dcVILP) 是已知的,但它们在未结合和受体结合状态下的结构尚未得到解决。我们报告了三种 dcVILP(dcGIV、dcSGIV 和 dcLCDV1)及其与受体(μIR、μIGF1R 和 μhybR)复合物的全原子结构模型,并使用全原子分子动力学 (MD) 模拟探测每个系统中的肽/受体相互作用。基于计算肽(胰岛素和 dcVILP)与受体之间每个残基的非键相互作用能,我们提供了关于建立重要相互作用的残基的详细信息。观察到的位点 1 胰岛素/μIR 相互作用与先前的实验研究一致,并且肽(胰岛素和 dcVILP)与受体的相互作用的残基级比较表明,由于序列差异,dcVILP 还建立了一些与胰岛素和 IR 之间的相互作用不同的相互作用。我们还设计了胰岛素类似物,并报告了一些类似物与受体之间增强的相互作用。