General Information


DRAVP ID  DRAVPe00681

Peptide Name   P-57

Sequence  WEQKIEELLKKAEEQQKKNEEEK

Sequence Length  23

UniProt ID  P03377 

Source  Synthetic construct



Activity Information


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>750 nM);
  • HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50>750 nM);
  • HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50>750 nM).

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

Cytotoxicity 

  • No cytotoxicity information or data found in the reference(s) presented in this entry

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)



Structure Information


PDB ID  None

Predicted Structure Download  DRAVPe00681

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C127H208N34O44

Absent amino acids  CDFGHMPRSTVY

Common amino acids  E

Mass  2915.25

Pl  4.94

Basic residues  6

Acidic residues  8

Hydrophobic residues  5

Net charge  -2

Boman Index  -9214

Hydrophobicity  -227.83

Aliphatic Index  55.22

Half Life 

  •     Mammalian:2.8 hour
  •     Yeast:3 min
  •     E.coli:2 min

Extinction Coefficient cystines  5500

Absorbance 280nm  250

Polar residues  1



Literature Information


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