School of Chemistry, National University of Ireland Galway, Galway, Ireland.
Biophys J. 2013 Jun 4;104(11):2503-11. doi: 10.1016/j.bpj.2013.04.023.
XPA is an essential protein in the nucleotide excision repair (NER) pathway, in charge of recruiting the ERCC1-XPF endonuclease complex to the DNA damage site. The only currently available structural insight into the binding of XPA to ERCC1 derives from the solution NMR structure of a complex between the ERCC1 central fragment and a 14-residue peptide, corresponding to the highly conserved binding motif of the XPA N-terminus, XPA₆₇₋₈₀. The extensive all-atom molecular-dynamics simulation study of the XPA₆₇₋₈₀ peptide both bound to the ERCC1 central fragment and free in solution presented here completes the profile of the structural determinants responsible for the ERCC1/XPA₆₇₋₈₀ complex stability. In addition to the wild-type, this study also looks at specific XPA₆₇₋₈₀ mutants in complex with the ERCC1 central domain and thus contributes to defining the conformational determinants for binding, as well as all of the essential structural elements necessary for the rational design of an XPA-based, ERCC1-specific inhibitor.
XPA 是核苷酸切除修复(NER)途径中的一种必需蛋白,负责将 ERCC1-XPF 内切酶复合物招募到 DNA 损伤部位。目前唯一可用的关于 XPA 与 ERCC1 结合的结构见解来自于 ERCC1 中心片段与 14 个残基肽之间复合物的溶液 NMR 结构,该肽对应于 XPA N 端高度保守的结合基序 XPA₆₇₋₈₀。本文中提出的对结合 ERCC1 中心片段的 XPA₆₇₋₈₀ 肽以及游离于溶液中的 XPA₆₇₋₈₀ 肽的全原子分子动力学模拟研究,完整描绘了决定 ERCC1/XPA₆₇₋₈₀ 复合物稳定性的结构决定因素。除了野生型,这项研究还研究了与 ERCC1 中心结构域结合的特定 XPA₆₇₋₈₀ 突变体,因此有助于确定结合的构象决定因素,以及基于 XPA 的、针对 ERCC1 的抑制剂的合理设计所需的所有基本结构要素。