General Information


DRAVP ID  DRAVPe00695

Peptide Name   P-75

Sequence  EMTWEEWEKKIEEYTKKIEEILKKSEEQQKKNEEELKKLEK

Sequence Length  41

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=0.9±0.2 nM);
  • HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=0.6±0.1 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  DRAVPe00695

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C233H377N57O77S

Absent amino acids  ACDFGHPRV

Common amino acids  E

Mass  5240.95

Pl  5.02

Basic residues  11

Acidic residues  14

Hydrophobic residues  8

Net charge  -3

Boman Index  -14626

Hydrophobicity  -197.32

Aliphatic Index  57.07

Half Life 

  •     Mammalian:1 hour
  •     Yeast:30 min
  •     E.coli:>10 hour

Extinction Coefficient cystines  12490

Absorbance 280nm  312.25

Polar residues  5



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