Stapled peptides are synthetic peptidomimetics of bioactive sites in folded proteins which carry chemical links, introduced during peptide synthesis, designed to retain the secondary structure in the native protein molecule. Stapled peptides have been investigated as potential modulators of protein–protein interactions for over two decades. The potential use of stapled peptides as inhibitors of viral entry, and therefore as antiviral therapeutics, has been established for several important viruses causing disease in humans, such as the human immunodeficiency virus type 1 (HIV-1), respiratory syncytial virus (RSV), and Middle East Respiratory Syndrome (MERS) coronavirus. Several independent research initiatives have investigated the inhibitory effect of stapled peptides on binding of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative agent of COVID-19, to its receptor, angiotensin-converting-enzyme 2 (ACE2). These stapled peptides, which mimic Helix 1 of the human ACE2 receptor, have demonstrated mixed ability to prevent infection with SARS-CoV-2 in cell-based studies.

中文翻译：

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钉合肽作为 SARS-CoV-2 与 hACE2 受体结合的潜在抑制剂

钉合肽是折叠蛋白质中生物活性位点的合成肽模拟物，其携带化学键，在肽合成过程中引入，旨在保留天然蛋白质分子中的二级结构。二十多年来，人们一直在研究钉合肽作为蛋白质-蛋白质相互作用的潜在调节剂。钉合肽作为病毒进入抑制剂的潜在用途，因此作为抗病毒治疗剂，已经确定用于导致人类疾病的几种重要病毒，例如人类免疫缺陷病毒 1 型 (HIV-1)、呼吸道合胞病毒 (RSV)和中东呼吸综合征 (MERS) 冠状病毒。一些独立的研究计划已经研究了钉合肽对严重急性呼吸综合征冠状病毒 2 (SARS-CoV-2) 结合的抑制作用，COVID-19 的病原体及其受体血管紧张素转换酶 2 (ACE2)。这些模拟人类 ACE2 受体的 Helix 1 的订书肽在基于细胞的研究中显示出混合预防 SARS-CoV-2 感染的能力。