General information
    ACovPid:ACoVP100178
    Trivial Name:PHI-AuNR
    Amino Acids Sequence:CGGGGGSLTEINTELLDLEYEMKKLEEVVKKLEESYIDLKEL-AuNR
    Length:42
    C-Terminal Modification:AuNR: gold nanorods;  
    N-Terminal Modification:None
    Chemical Modification:None
    Peptide Source:

    The Middle East respiratory syndrome coronavirus (MERS-CoV) :

    Source Description:PIH was synthesized with the standard solid-phase procedure,15purified by HPLC, and identified by LC−ESI−MS. VP-ODS C18 column (150×4.6 mm2,5µm) was used for theHPLC analyses. The solvent A (0.1% trifluoroacetic acid (TFA) in100% water (v/v)) and solvent
    Against Virus:

    The Middle East respiratory syndrome coronavirus (MERS-CoV)

    Inhibition Value Type:IC50
    Inhibitory Effect:1.171
    Inhibitory Unit:µM
    Target Domain Name:
    Assay:Cell-cell fusion
    Assay Description:MERS-CoV S2 Subunit-Mediated Cell Fusion Model:293Tcells were transfected with the plasmid of either pAAV-IRES-MERS-EGFP or pAAV-IRES-EGFP and cultured at 37°C for 36 h,generating 293T/MERS/EGFP and 293T/EGFP, respectively. Huh-7cells (5×10^4) were incubated in 96-well microplates at 37°C for 12h, followed by adding 2×104293T/EGFP or 293T/MERS/EGFPcells. The cell fusion was imaged using an invertedfluorescencemicroscope at different time points (0, 1, 2, 3, 4, 5, 6, 8, and 12 h).The fused cells were identified by measuring the enhanced greenfluorescent protein (EGFP)fluorescence intensity, which is at least 1-fold lower in fused cells than intact cells. The number of cell fusionswas calculated using the Image J software. The fusion rates (F) werecalculated using the following formula:N/T×100%, where“N”represents the number of fused cells and“T”represents the totalnumber of 293T cells. Inhibition of MERS-CoV S2 Subunit-Mediated Cell Fusion : 293T/MERS/EGFP or 293T/EGFP cells (2×10^4) were pretreatedwith HR1 inhibitors for 30 min and then added into the Huh-7 cells(5×10^4). After co-culture at 37°C for 6 h, the cell fusions wereimaged using afluorescence microscope. The number of cell fusionswere calculated using the Image J software. The fusion rates (FP,FH,FN) were calculated using the following formula:F/A×100%, where“F”represents the number of fused cells,“A”represents the totalnumber of 293T cells,“FP”represents the cell fusion rate between293T/MERS/EGFP and Huh-7 cells in the absence of HR1inhibitors,“FH”represents the cell fusion rate between 293T/MERS/EGFP cells and Huh-7 cells in the presence of HR1 inhibitors,“FN”represents the cell fusion rate between 293T/EGFP cells andHuh-7 cells in the absence of HR1 inhibitors. The inhibition rate (I)of cell fusions was calculated using the following formula: (FP−FH)/(FP−FN)×100%. The concentration for 50% inhibition (IC50) wascalculated using the IBM SPSS software. MERS-CoV infects the host cells through S2 subunitinduced membrane fusion : During infections, the HR1 and HR2 domains in the S2 subunit form a 6-HB fusion core, which is responsive for membrane fusion between MERS-CoV and host cells. Therefore, inhibiting the formation of 6-HB is a promising method against MERS-CoV infections. However, MERS-CoV belongs to a family of viruses that can infect a variety of mammalian hosts and is readily transmissible among humans by direct contact with respiratory secretions, body fluids, and excretions from infected individuals. Consequently, the containment level 3 is required for all in vitro and in vivo studies, significantly hindering the development of anti-MERS treatments. We therefore constructed the cell fusion model to systemically evaluate the therapeutic efficacy of anti-MERS agents. It has been reported that Huh-7 cells showed higher susceptibility to MERS-CoV than respiratory tract cells, and, therefore, we constructed the cell fusion model with 293T cells co-expressed with EGFP/S protein and Huh-7 cells with MERS-CoV receptor DPP4. We thus performed the experiments to verify whether PIH could inhibit the cell fusion mediated by S2 subunit. The cellular size of 293T cells (MERS/EGFP) increased after fusing with Huh-7 cells, and the fused cells showed at least 2-fold lower fluorescence intensity compared to that of 293T cells (EGFP) (Figure 4a), indicating that S proteins on the 293T cells could recognize DPP4 on Huh-7 cells to induce cell fusion. In addition, we further identified that cell fusion between 293T and Huh-7 cells showed time-dependence, and reached the plateau after 6h (Figure 4b). Based on this established cell fusion model, we further investigated the inhibitory effects of PIH on S2 subunit-mediated cell fusion at 6 h after co-culture. Figure 4c,d shows that PIH had a dose-dependent responding profile with IC50 of 1.171 µM and could completely inhibit the cell fusion at a concentration of 10 µM, indicating that PIH has a high inhibitory activity for MERS-CoV infections.
    Anti-CoV activity in vivo:
    Reference:31099550
    Comment:
    3D structure:

    Structure Experiment Verified:
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