DRAVP ID  DRAVPe00787

Peptide Name   LP-83

Sequence  WEQKIEELLKKAEEQQKKNEEELKKLEKX

Sequence Length  29

UniProt ID  P03377 

Source  Synthetic construct

Target Organism  HIV,SIV

Assay  cell-fusion assay,single-cycle infection assay

Activity 

• [Ref.30867304]HIV-1 NL4-3(X4):inhibition of virus replication in TZM-bl cells(IC50=0.49±0.03 pM);
• HIV-1 JR-CSF(R5):inhibition of virus replication in TZM-bl cells(IC50=4.54±1.42 pM);
• HIV-1 89.6(R5X4):inhibition of virus replication in TZM-bl cells(IC50=4.75±0.83 pM);
• HIV-1 pseudovirus:inhibition of pseudovirus infection in TZM-bl cells(IC50=2.91 pM);
• T-20 sensitive HIV-1(NL4-3D36G):inhibition of virus infection in TZM-bl cells(IC50=0.002±0 nM);
• T-20 resistant HIV-1 NL4-3(WT,I37T,V38A,V38 M,Q40H,N43K,G36S/V38 M,I37T/N43K,V38A/N42T):inhibition of virus infection in TZM-bl cells(IC50=0.002-0.041 nM);
• HIV-2(ROD,ST):inhibition of virus infection in TZM-bl cells(IC50=0.02-0.032 nM);
• SIV(239,PBJ):inhibition of virus infection in TZM-bl cells(IC50=0.004-0.006 nM);
• HIV-1(1A,2B,1C,1G,1A/C,1A/E,1B/C subtype):inhibition of cell-cell fusion between HEK293T cells and TZM-bl cells(IC50=8.55 pM).

Hemolytic Activity  No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity 

• [Ref.30867304]Human PBMC:CC50=40.27 µM;
• Human embryonic kidney HEK293T cells:CC50=25.31 µM;
• TZM-bl cells:CC50=12.34 μM;
• MT-4 cells:CC50=19.65 μM;
• C8166 cells:CC50=19.19 μM;
• U937 cells:CC50=9.97 μ

Binding Target  membrane

Mechanism  The peptide had extremely potent activity to block HIV envelope-mediated cell-cell fusion,showing a greatly increased potency relative to its inhibition on virus infection. Besides, it efficiently bounds to both the cellular and viral membranes to exert their antiviral activities.

PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  The 'X' at position 29 is Cys-Chol(cholesterol)

Stereochemistry  L

Literature 1

Title   Design and Characterization of Cholesterylated Peptide HIV-1/2 Fusion Inhibitors with Extremely Potent and Long-Lasting Antiviral Activity.

Pubmed ID   30867304

Reference   J Virol. 2019 May 15;93(11):e02312-18.

Author   Zhu Y, Chong H, Yu D, Guo Y, Zhou Y, He Y.

DOI   10.1128/JVI.02312-18