General Information


DRAVP ID  DRAVPe00605

Peptide Name   MT-SC23EK

Sequence  MTWEEWDKKIEEYTKKIEELIKKSE

Sequence Length  25

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=2.1±0.2 nM);
  • HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=1.9±0.7 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  DRAVPe00605

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C146H229N33O46S

Absent amino acids  ACFGHNPQRV

Common amino acids  E

Mass  3214.68

Pl  4.9

Basic residues  6

Acidic residues  8

Hydrophobic residues  6

Net charge  -2

Boman Index  -7168

Hydrophobicity  -150

Aliphatic Index  62.4

Half Life 

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

Extinction Coefficient cystines  12490

Absorbance 280nm  520.42

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