Table 4 Proteinaceous inhibitors blocking the HR1-HR2 interaction
Name | Constructs | IC50s of viral S-mediated cell-cell fusion (nM) | IC50s of pseudotyped coronaviruses (nM) | IC50s of Live coronaviruses (nM) | Protective efficacy | Refs. |
|---|---|---|---|---|---|---|
HR1MFd | HR1(E918-V952)-Fd | WT: 740 | WT: 1230, Alpha: 2350, Omicron: 1060, SARS-CoV: 2130, MERS-CoV: 2860 | N.A. | N.A. | |
5-HB-H2 | HR1-HR2-HR1-HR2-HR1-His (HR1:E918-L966; HR2: D1168-L1203) | SARS-CoV-2: 630 | WT: 590, Beta: 3080, Omicron: 1630, Kappa: 3250, Delta: 2660, RaTG13: 2510, PANG/GD: 1.0, SARS-CoV: 1670, WIV1: 2460, HKU3: 1.0 | N.A. | N.A. | |
SARS-CoV-2-5-Helix | HR1-HR2-HR1-HR2-HR1-His (HR1:L922-Q965; HR2: D1165-G1204) | SARS-CoV-2: 127 | WT: 243, Alpha: 363.6, Beta: 169.7, Gamma (P.1): 141.8, Delta: 368.9, Omicron: 140.7, lambda: 238.2 | SARS-CoV-2: 293, Omicron: 279 | N.A. | |
GL25E | GRFT-(G4S)5-EK1 | SARS-CoV-2: 4.4, SARS-CoV: 30.1, MERS-CoV: 4.9, HCoV-NL63: 0.40, HCoV-229E: 0.33, HCoV-OC43: 0.27 | WT: 8.7, SARS-CoV: 62.1, MERS-CoV: 0.2, HCoV-NL63: 0.5, HCoV-229E: 1.8, HCoV-OC43: 0.15 | SARS-CoV-2: 29.8, HCoV-OC43: 0.2, HCoV-229E: 177.2 | Intranasal application of GL25E can prevent and treat infection in mice challenged with HCoV-OC43 | |
FL-EK1 | FN3-Linker-EK1 | SARS-CoV-2: 68.5 HCoV-OC43: 398.2 | WT: 90.6, Alpha: 114.5, Beta: 201.2, Gamma (P.1): 373.1, Delta: 133.0, Omicron: 297.5, Lambda: 88.5, Eta: 179.2, Kappa: 230.9, HCoV-OC43: 1593 | SARS-CoV-2: 25.3, Delta: 281.2, HCoV-OC43: 207 | Intranasal application of FL-EK1 can prevent and treat infection in mice challenged with HCoV-OC43 and SARS-CoV-2 Delta variant |
