DRAVP ID  DRAVPe00678

Peptide Name   P-52

Sequence  WEQKIEELLKKAEEQQKKNEEELKKLEK

Sequence Length  28

UniProt ID  P03377 

Source  Synthetic construct

Target Organism  HIV

Assay  cell-fusion assay,single-cycle infection assay

Activity 

• [Ref.30089693]HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=0.9±0.1 nM);
• HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=1.9±0.6 nM);
• HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=1.9±0.4 nM);
• HIV-1(3 A, 13 B, 7 C, 1 G, 1 A/C, 5 A/E, 6 B/C pseudovirus subtypes):inhibition of pseudovirus infection in TZM-bl cells(IC50=20541 pM).

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

Cytotoxicity 

• [Ref.30089693]TZM-bl cell:CC50=916.6 ±42.46 μM;
• MT-4 cell:CC50=770.63±131.46 μM;
• HEK293T cell:CC50=649.07± 37.03μM;
• PBMC:CC50=91.19± 20.46 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  DRAVPe00678

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

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