DRAVP ID  DRAVPe00783

Peptide Name   LP-50

Sequence  YTSLIEELIKKSEEQQKKNEEELKKLEX

Sequence Length  28

UniProt ID  P03377 

Source  Synthetic construct

Target Organism  HIV,SIV

Assay  cell-fusion assay,single-cycle infection assay

Activity 

• [Ref.30089693]HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=21±3 pM);
• HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=7±1 pM);
• HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=23±2 pM);
• T-20 sensitive HIV-1(NL4-3D36G):inhibition of virus infection in TZM-bl cells(IC50<0.01 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=0.06-136.12 nM);
• HIV-2(ROD,ST):inhibition of virus infection in TZM-bl cells(IC50=0.09-5.81 nM);
• SIV(239,PBJ):inhibition of virus infection in TZM-bl cells(IC50=0.06 nM).

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

Cytotoxicity 

• [Ref.30089693]TZM-bl cell:CC50=106.4 ± 2.72 μM;
• MT-4 cell:CC50=138.37± 6.55 μM;
• HEK293T cell:CC50=166.77± 35.33μM;
• PBMC:CC50=40.01± 4.63 μM.

Binding Target  membrane

Mechanism  The peptide acts by binding to the heptad repeat 1 (HR1) region of gp41 and preventing the interaction of the HR1 and HR2 domains, which is required for virus–cell fusion.(By similar)

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 28 is Lys-C16(palmitic acid)

Stereochemistry  L

Literature 1

Title   Structural and Functional Characterization of Membrane Fusion Inhibitors with Extremely Potent Activity against Human Immunodeficiency Virus Type 1 (HIV-1), HIV-2, and Simian Immunodeficiency Virus.

Pubmed ID   30089693

Reference   J Virol. 2018 Sep 26;92(20):e01088-18.

Author   Chong H, Zhu Y, Yu D, He Y.

DOI   10.1128/JVI.01088-18