Department of Structural Biology, The Weizmann Institute of Science, Rehovot 7610001, Israel.
The Ilana and Pascal Mantoux Institute for Bioinformatics, The Nancy and Stephen Grand Israel National Center for Personalized Medicine, Weizmann Institute of Science, Rehovot 7610001, Israel.
Structure. 2017 Aug 1;25(8):1233-1241.e3. doi: 10.1016/j.str.2017.06.004. Epub 2017 Jul 6.
Erythromycin is a clinically useful antibiotic that binds to an rRNA pocket in the ribosomal exit tunnel. Commonly, resistance to erythromycin is acquired by alterations of rRNA nucleotides that interact with the drug. Mutations in the β hairpin of ribosomal protein uL22, which is rather distal to the erythromycin binding site, also generate resistance to the antibiotic. We have determined the crystal structure of the large ribosomal subunit from Deinococcus radiodurans with a three amino acid insertion within the β hairpin of uL22 that renders resistance to erythromycin. The structure reveals a shift of the β hairpin of the mutated uL22 toward the interior of the exit tunnel, triggering a cascade of structural alterations of rRNA nucleotides that propagate to the erythromycin binding pocket. Our findings support recent studies showing that the interactions between uL22 and specific sequences within nascent chains trigger conformational rearrangements in the exit tunnel.
红霉素是一种临床上有用的抗生素,它与核糖体出口通道中的 rRNA 口袋结合。通常,通过与药物相互作用的 rRNA 核苷酸的改变来获得对红霉素的耐药性。核糖体蛋白 uL22 的β发夹中的突变,该突变位于红霉素结合位点相当远的位置,也会产生对抗生素的耐药性。我们已经确定了来自 Deinococcus radiodurans 的大亚基核糖体的晶体结构,其中 uL22 的β发夹内有三个氨基酸插入,使该蛋白对红霉素产生耐药性。该结构揭示了突变的 uL22 的β发夹向出口通道内部的移位,引发 rRNA 核苷酸的一系列结构改变,这些改变会传播到红霉素结合口袋。我们的发现支持了最近的研究,表明 uL22 与新生链内特定序列之间的相互作用会引发出口通道中的构象重排。