General Information


DRAVP ID  DRAVPe00581

Peptide Name   SC30EK

Sequence  WEEWDKKIEEYTKKIEELIKKSEEQQKKNE

Sequence Length  30

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±0 nM);
  • HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=0.9±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 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  DRAVPe00581

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C173H273N43O57

Absent amino acids  ACFGHMPRV

Common amino acids  E

Mass  3867.32

Pl  5.03

Basic residues  8

Acidic residues  10

Hydrophobic residues  6

Net charge  -2

Boman Index  -11390

Hydrophobicity  -213.33

Aliphatic Index  52

Half Life 

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

Extinction Coefficient cystines  12490

Absorbance 280nm  430.69

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