IrsiCaixa Acquired Immune Deficiency Syndrome Research Institute, Badalona 08916, Spain.
Laboratory of Molecular Virology, Institute of Biology, Department of Genetics, Federal University of Rio de Janeiro, Rio de Janeiro 21941-90, Brazil.
Proc Natl Acad Sci U S A. 2023 Mar 7;120(10):e2214561120. doi: 10.1073/pnas.2214561120. Epub 2023 Feb 28.
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is an enveloped positive stranded RNA virus which has caused the recent deadly pandemic called COVID-19. The SARS-CoV-2 virion is coated with a heavily glycosylated Spike glycoprotein which is responsible for attachment and entry into target cells. One, as yet unexploited strategy for preventing SARS-CoV-2 infections, is the targeting of the glycans on Spike. Lectins are carbohydrate-binding proteins produced by plants, algae, and cyanobacteria. Some lectins can neutralize enveloped viruses displaying external glycoproteins, offering an alternative therapeutic approach for the prevention of infection with virulent β-coronaviruses, such as SARS-CoV-2. Here we show that the cyanobacterial lectin cyanovirin-N (CV-N) can selectively target SARS-CoV-2 Spike oligosaccharides and inhibit SARS-CoV-2 infection in vitro and in vivo. CV-N neutralizes Delta and Omicron variants in vitro better than earlier circulating viral variants. CV-N binds selectively to Spike with a Kd as low as 15 nM and a stoichiometry of 2 CV-N: 1 Spike but does not bind to the receptor binding domain (RBD). Further mapping of CV-N binding sites on Spike shows that select high-mannose oligosaccharides in the S1 domain of Spike are targeted by CV-N. CV-N also reduced viral loads in the nares and lungs in vivo to protect hamsters against a lethal viral challenge. In summary, we present an anti-coronavirus agent that works by an unexploited mechanism and prevents infection by a broad range of SARS-CoV-2 strains.
严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)是一种包膜的正链 RNA 病毒,导致了最近致命的 COVID-19 大流行。SARS-CoV-2 病毒体被一层富含糖基的 Spike 糖蛋白覆盖,该糖蛋白负责附着和进入靶细胞。一种尚未开发的预防 SARS-CoV-2 感染的策略是针对 Spike 上的聚糖。凝集素是植物、藻类和蓝细菌产生的糖结合蛋白。一些凝集素可以中和显示外部糖蛋白的包膜病毒,为预防诸如 SARS-CoV-2 等毒力β冠状病毒的感染提供了另一种治疗方法。在这里,我们表明蓝细菌凝集素 cyanovirin-N(CV-N)可以选择性地针对 SARS-CoV-2 Spike 寡糖并抑制 SARS-CoV-2 在体外和体内的感染。CV-N 在体外比早期循环的病毒变异体更好地中和 Delta 和奥密克戎变异体。CV-N 以低至 15 nM 的 Kd 选择性地结合 Spike,结合比为 2 CV-N:1 Spike,但不结合受体结合域(RBD)。对 Spike 上 CV-N 结合位点的进一步作图表明,CV-N 靶向 Spike 中 S1 结构域的一些高甘露糖寡糖。CV-N 还降低了体内鼻腔和肺部的病毒载量,以保护仓鼠免受致命病毒的攻击。总之,我们提出了一种通过未开发的机制起作用的抗冠状病毒药物,并预防广泛的 SARS-CoV-2 株感染。