表位
肽
圆二色性
化学
重组DNA
螺旋(腹足类)
穗蛋白
严重急性呼吸综合征冠状病毒2型(SARS-CoV-2)
蛋白质二级结构
生物化学
生物物理学
2019年冠状病毒病(COVID-19)
立体化学
生物
抗体
医学
传染病(医学专业)
免疫学
疾病
病理
蜗牛
基因
生态学
作者
Lorenzo Calugi,Giulia Sautariello,Elena Lenci,Andrea Trabocchi
标识
DOI:10.26434/chemrxiv-2022-xpqfh
摘要
The design and synthesis of a series of peptide derivatives based on a short ACE2 alpha-helix 1 epitope and subsequent [i - i+4] stapling of the secondary structure resulted in the identification of a 9-mer peptide capable to compete with recombinant ACE2 towards Spike RBD in the micromolar range. Specifically, SARS-CoV-2 Spike inhibitor screening based on colorimetric ELISA assay and structural studies by circular dichroism showed the ring-closing metathesis cyclization being capable to stabilize the helical structure of the 9-mer 34-HEAEDLFYQ-42 epitope better than the triazole stapling via click chemistry. The results are preliminary for the development of small molecule stapled peptides capable of blocking the key ACE2-Spike S1 protein-protein interaction.
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