Jørgensen Rene, Ortiz Pedro A, Carr-Schmid Anne, Nissen Poul, Kinzy Terri Goss, Andersen Gregers Rom
Department of Molecular Biology, Aarhus University, Gustav Wieds vej 10C, DK8000 Arhus, Denmark.
Nat Struct Biol. 2003 May;10(5):379-85. doi: 10.1038/nsb923.
Two crystal structures of yeast translation elongation factor 2 (eEF2) were determined: the apo form at 2.9 A resolution and eEF2 in the presence of the translocation inhibitor sordarin at 2.1 A resolution. The overall conformation of apo eEF2 is similar to that of its prokaryotic homolog elongation factor G (EF-G) in complex with GDP. Upon sordarin binding, the three tRNA-mimicking C-terminal domains undergo substantial conformational changes, while the three N-terminal domains containing the nucleotide-binding site form an almost rigid unit. The conformation of eEF2 in complex with sordarin is entirely different from known conformations observed in crystal structures of EF-G or from cryo-EM studies of EF-G-70S complexes. The domain rearrangements induced by sordarin binding and the highly ordered drug-binding site observed in the eEF2-sordarin structure provide a high-resolution structural basis for the mechanism of sordarin inhibition. The two structures also emphasize the dynamic nature of the ribosomal translocase.
测定了酵母翻译延伸因子2(eEF2)的两种晶体结构:分辨率为2.9 Å的无配体形式以及分辨率为2.1 Å的在转位抑制剂梭链孢酸存在下的eEF2结构。无配体eEF2的整体构象与其与GDP结合的原核同源延伸因子G(EF-G)相似。梭链孢酸结合后,三个模拟tRNA的C端结构域发生显著构象变化,而包含核苷酸结合位点的三个N端结构域形成一个几乎刚性的单元。与梭链孢酸结合的eEF2构象与EF-G晶体结构中观察到的已知构象或EF-G-70S复合物的冷冻电镜研究结果完全不同。梭链孢酸结合诱导的结构域重排以及在eEF2-梭链孢酸结构中观察到的高度有序的药物结合位点为梭链孢酸抑制机制提供了高分辨率的结构基础。这两种结构还强调了核糖体转位酶的动态性质。