General Information


DRAVP ID  DRAVPe00654

Peptide Name   LP-59

Sequence  WEQKIEELLKKAEEQQKX

Sequence Length  18

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>900000 pM);
  • HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=240800±23649 pM);
  • HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=210477±25537 pM).

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  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  The 'X' at position 18 is Lys-C16(palmitic acid)

Stereochemistry  L



Physicochemical Information


Formula  C96H155N25O30

Absent amino acids  CDFGHMNPRSTVY

Common amino acids  E

Mass  2268.78

Pl  5.07

Basic residues  4

Acidic residues  5

Hydrophobic residues  5

Net charge  -1

Boman Index  -5397

Hydrophobicity  -170

Aliphatic Index  70.56

Half Life 

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

Extinction Coefficient cystines  5500

Absorbance 280nm  323.53

Polar residues  0



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