Table 1.
Sequences and properties of synthesized peptides.
Code | Sequencea | Predicted helical content%b | Predicted antigenicity (AD)c | Experimental helical content%d | % Inhibition of SARSCoV-2 replication at 10 μMe | SARSCoV-2 virus titer at 1 μM (PFU mL−1) on Calu-3f | IC50 (nM)g Calu-3 | KDh (nM) |
---|---|---|---|---|---|---|---|---|
P1 | STIEE QAKTF LDKFN HEAED LFYQS SL-NH2 | 6 | 0 | 7 | 9 | – | – | – |
P1scr | AHLFS YLTTK EEQDN DAIFL QEFSK ES-NH2 | 1 | 0 | 8 | 7 | – | – | – |
Ppen | IEE QAKTF LDKFN HEAED LFYQS-NH2 | 1 | 0 | 10 | 14 | – | – | – |
P2 | SALEE QLKTF LDKFL HELED LLYQL SL-NH2 | 64 | 1 | 70 | 16 | – | – | – |
P3 | SALEE QLKTF LDKFL HELED LLYQL AL-NH2 | 78 | 1 | 64 | 4 | – | – | – |
P4 | Ac-SALEE QLKTF LDKFL HELED LLYQL AL-NH2 | 66 | 1 | 70 | 24 | – | – | – |
P5 | SALEE QLKTF LDKFL HELED PLYQL AL-NH2 | 34 | 1 | 17 | 27 | – | – | – |
P6 | SALEE QLKTF LDKFL HELED LLYQL ALAL-NH2 | 88 | 1 | 80 | 6,5 | – | – | – |
P7 | SALEE QYKTF LDKFL HELED LLYQL ALAL-NH2 | n.a. | n.a. | 63 | 54 | – | – | – |
P8 | SALEE QLKTF LDKFM HELED LLYQL AL-NH2 | 68 | 0 | 70 | 91 | 0 | 46 | 24 ± 11 |
P9 | SALEE QYKTF LDKFM HELED LLYQL SL-NH2 | n.a. | n.a. | 53 | 93 | 0 | 53 | 0.09 ± 0.08 |
P10 | SALEE QYKTF LDKFM HELED LLYQL AL-NH2 | n.a. | n.a. | 56 | 95 | 0 | 42 | 0.03 ± 0.01 |
aThe homotyrosine residue is depicted with the underlined letter Y in peptides P7, P9, and P10.
bPredicted helical content using Agadir program available at https://agadir.crg.es; n.a., not applicable (for hTyr containing sequences).
cPredicted antigenicity calculated at http://imed.med.ucm.es/Tools/antigenic.pl; n.a., not applicable (for hTyr containing sequences).
dExperimental helical content determined by circular dichroism (see Fig. 2).
eMean percentage of inhibition on Vero-E6 cells of at least three independent experiments (see Fig. 3a and Supplementary Fig. 3).
fMean viral titration on Calu-3 cells (see Fig. 3d (Fig. 3b for Vero-E6 cells)).
ggIC50 determined on Calu-3 cells only for peptides able to inhibit SARSCoV-2 cell infection.
hDissociation constants with SARS-Cov-2 RBD-SD1 measured by BLI for peptides with IC50 in the nM range. KD values are the mean of three independent determinations (P9 and P10).