University of Southern Denmark, Department of Physics, Chemistry and Pharmacy, Campusvej 55, 5230 Odense, Denmark.
Chem Commun (Camb). 2021 Apr 4;57(26):3283-3286. doi: 10.1039/d0cc08387a. Epub 2021 Mar 2.
SARS-CoV-2 Spike protein RBD interacts with the hACE2 receptor to initiate cell entry and infection. We set out to develop lactam-based i,i + 4 stapled hACE2 peptides targeting SARS-CoV-2. In vitro screening demonstrates the inhibition of the Spike protein RBD-hACE2 complex formation by the hACE2A36K-F40E stapled peptide (IC: 3.6 μM, K: 2.1 μM), suggesting that hACE2 peptidomimetics could form the basis for the development of anti-COVID-19 therapeutics.
SARS-CoV-2 的刺突蛋白 RBD 与 hACE2 受体相互作用，从而启动细胞进入和感染。我们着手开发基于内酰胺的 i,i + 4 订书钉 hACE2 肽，以靶向 SARS-CoV-2。体外筛选表明，hACE2A36K-F40E 订书钉肽抑制刺突蛋白 RBD-hACE2 复合物的形成（IC：3.6 μM，K：2.1 μM），这表明 hACE2 肽模拟物可能成为开发抗 COVID-19 疗法的基础。
