Department of Economics, University of Ioannina, 45110 Ioannina, Greece.
J Mol Model. 2011 Jul;17(7):1817-29. doi: 10.1007/s00894-010-0884-4. Epub 2010 Nov 16.
Human MUC1 is over-expressed in human adenocarcinomas and has been used as a target for immunotherapy studies. The 9-mer MUC1-9 peptide has been identified as one of the peptides which binds to murine MHC class I H-2K(b). The structure of MUC1-9 in complex with H-2K(b) has been modeled and simulated with classical molecular dynamics, based on the x-ray structure of the SEV9 peptide/H-2K(b) complex. Two independent trajectories with the solvated complex (10 ns in length) were produced. Approximately 12 hydrogen bonds were identified during both trajectories to contribute to peptide/MHC complex, as well as 1-2 water mediated hydrogen bonds. Stability of the complex was also confirmed by buried surface area analysis, although the corresponding values were about 20% lower than those of the original x-ray structure. Interestingly, a bulged conformation of the peptide's central region, partially characterized as a β-turn, was found exposed form the binding groove. In addition, P1 and P9 residues remained bound in the A and F binding pockets, even though there was a suggestion that P9 was more flexible. The complex lacked numerous water mediated hydrogen bonds that were present in the reference peptide x-ray structure. Moreover, local displacements of residues Asp4, Thr5 and Pro9 resulted in loss of some key interactions with the MHC molecule. This might explain the reduced affinity of the MUC1-9 peptide, relatively to SEV9, for the MHC class I H-2K(b).
人 MUC1 在人类腺癌中过度表达,并已被用作免疫治疗研究的靶标。9 肽 MUC1-9 已被鉴定为与鼠 MHC 类 I H-2K(b)结合的肽之一。基于 SEV9 肽/H-2K(b)复合物的 X 射线结构,使用经典分子动力学对 MUC1-9 与 H-2K(b)的复合物结构进行了建模和模拟。生成了两个含有溶剂的复合物的独立轨迹(长度为 10ns)。在两条轨迹中都鉴定出了大约 12 个氢键,这些氢键有助于肽/MHC 复合物的形成,以及 1-2 个水介导的氢键。通过埋藏表面积分析也证实了复合物的稳定性,尽管相应的值比原始 X 射线结构低约 20%。有趣的是,发现肽的中心区域的凸起构象,部分特征为β-转角,从结合槽中暴露出来。此外,即使 P9 更灵活,P1 和 P9 残基仍留在 A 和 F 结合袋中结合。该复合物缺乏存在于参考肽 X 射线结构中的许多水介导氢键。此外,残基 Asp4、Thr5 和 Pro9 的局部位移导致与 MHC 分子的一些关键相互作用丧失。这可能解释了 MUC1-9 肽相对于 SEV9 对 MHC 类 I H-2K(b)的亲和力降低。