General Information


DRAVP ID  DRAVPe00694

Peptide Name   P-74

Sequence  WEEWEKKIEEYTKKIEEILKKSEEQQKKNEEELKKLEK

Sequence Length  38

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=0.4±0.1 nM);
  • HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=0.8±0.1 nM);
  • HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=1.4±0.4 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  DRAVPe00694

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C219H354N54O71

Absent amino acids  ACDFGHMPRV

Common amino acids  E

Mass  4879.54

Pl  5.19

Basic residues  11

Acidic residues  13

Hydrophobic residues  8

Net charge  -2

Boman Index  -13923

Hydrophobicity  -206.84

Aliphatic Index  61.58

Half Life 

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

Extinction Coefficient cystines  12490

Absorbance 280nm  337.57

Polar residues  4



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