General Information


DRAVP ID  DRAVPe00598

Peptide Name   MT-SC30EK

Sequence  MTWEEWDKKIEEYTKKIEELIKKSEEQQKKNE

Sequence Length  32

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=0.8±0.1 nM);
  • HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=0.8±0.2 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  DRAVPe00598

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C182H289N45O60S

Absent amino acids  ACFGHPRV

Common amino acids  E

Mass  4099.62

Pl  5.03

Basic residues  8

Acidic residues  10

Hydrophobic residues  6

Net charge  -2

Boman Index  -11412

Hydrophobicity  -196.25

Aliphatic Index  48.75

Half Life 

  •     Mammalian:30 hour
  •     Yeast:>20 hour
  •     E.coli:>10 hour

Extinction Coefficient cystines  12490

Absorbance 280nm  402.9

Polar residues  5



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