General Information


DRAVP ID  DRAVPe00578

Peptide Name   SC33EK

Sequence  WEEWDKKIEEYTKKIEELIKKSEEQQKKNEKEL

Sequence Length  33

UniProt ID  Q5DP94 

Source  Synthetic construct



Activity Information


Target Organism  HIV

Assay  dual split-protein (DSP)-based cell-cell fusion assay,luciferase assay

Activity 

  • [Ref.31277353]HIV-1 NL4-3:inhibition of pseudovirus entry in TZM-bl cells(IC50=1.1±0.1 nM);
  • HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=0.7±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 inhibits HIV fusion by binding to the hydrophobic grooves on the N-terminal heptad repeat (NHR) trimer and blocking six-helix-bundle (6-HB) formation.



Structure Information


PDB ID  None

Predicted Structure Download  DRAVPe00578

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C190H303N47O62

Absent amino acids  ACFGHMPRV

Common amino acids  E

Mass  4237.77

Pl  5.08

Basic residues  9

Acidic residues  11

Hydrophobic residues  7

Net charge  -2

Boman Index  -12134

Hydrophobicity  -204.85

Aliphatic Index  59.09

Half Life 

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

Extinction Coefficient cystines  12490

Absorbance 280nm  390.31

Polar residues  4



Literature Information


Literature 1

Title   Conserved Residue Asn-145 in the C-Terminal Heptad Repeat Region of HIV-1 gp41 is Critical for Viral Fusion and Regulates the Antiviral Activity of Fusion Inhibitors.

Pubmed ID   31277353

Reference   Viruses. 2019 Jul 3;11(7):609. 

Author   Geng X, Liu Z, Yu D, Qin B, Zhu Y, Cui S, Chong H, He Y.

DOI   10.3390/v11070609