七肽的选择，其与细菌 23S 核糖体 RNA 的螺旋 69 结合。
Selection of heptapeptides that bind helix 69 of bacterial 23S ribosomal RNA.
机构信息
Department of Chemistry, Wayne State University, Detroit, MI 48202, USA.
出版信息
Bioorg Med Chem. 2013 Mar 1;21(5):1240-7. doi: 10.1016/j.bmc.2012.12.048. Epub 2013 Jan 10.
Helix 69 of Escherichia coli 23S rRNA has important roles in specific steps of translation, such as subunit association, translocation, and ribosome recycling. An M13 phage library was used to identify peptide ligands with affinity for helix 69. One selected sequence, NQVANHQ, was shown through a bead assay to interact with helix 69. Electrospray ionization mass spectroscopy revealed an apparent dissociation constant for the amidated peptide and helix 69 in the low micromolar range. This value is comparable to that of aminoglycoside antibiotics binding to the A site of 16S rRNA or helix 69. Helix 69 variants (human) and unrelated RNAs (helix 31 or A site of 16S rRNA) showed two- to fourfold lower affinity for NQVANHQ-NH(2). These results suggest that the peptide has desirable features for development as a lead compound for novel antimicrobials.
大肠杆菌 23S rRNA 的螺旋 69 在翻译的特定步骤中发挥着重要作用，例如亚基结合、易位和核糖体回收。我们使用 M13 噬菌体文库来鉴定与螺旋 69 具有亲和力的肽配体。通过珠粒分析，选择序列 NQVANHQ 显示与螺旋 69 相互作用。电喷雾电离质谱揭示了酰胺化肽和螺旋 69 的表观解离常数在低微摩尔范围内。该值与结合到 16S rRNA 或螺旋 69 A 位的氨基糖苷类抗生素的结合相当。螺旋 69 变体（人）和无关 RNA（螺旋 31 或 16S rRNA 的 A 位）对 NQVANHQ-NH(2) 的亲和力低两到四倍。这些结果表明，该肽具有作为新型抗菌药物先导化合物的理想特性。
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