The development of peptide ligands that target helix 69 rRNA of bacterial ribosomes.
The development of peptide ligands that target helix 69 rRNA of bacterial ribosomes.
复制标题
开发针对细菌核糖体螺旋 69 rRNA 的肽配体。
DOI：
10.1016/j.bmc.2016.07.050
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发表时间：
2016
影响因子：
3.5
通讯作者：
Chow,ChristineS
中科院分区：
文献类型：
--
作者：
Dremann,DanielleN;Chow,ChristineS
Antibiotic resistance prevents successful treatment of common bacterial infections, making it clear that new target locations and drugs are required to resolve this ongoing challenge. The bacterial ribosome is a common target for antibacterials due to its essential contribution to cell viability. The focus of this work is a region of the ribosome called helix 69 (H69), which was recently identified as a secondary target site for aminoglycoside antibiotics. H69 has key roles in essential ribosomal processes such as subunit association, ribosome recycling, and tRNA selection. Conserved across phylogeny, bacterial H69 also contains two pseudouridines and one 3-methylpseudouridine. Phage display revealed a heptameric peptide sequence that targeted H69. Using solid-phase synthesis, peptide variants with higher affinity and improved selectivity to modified H69 were generated. Electrospray ionization mass spectrometry was used to determine relative apparent dissociation constants of the RNA–peptide complexes.
