General Information


DRAVP ID  DRAVPe00608

Peptide Name   MT-SC20EK

Sequence  MTWEEWDKKIEEYTKKIEELIK

Sequence Length  22

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=3.7±0.5 nM);
  • HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=3.3±1.4 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  DRAVPe00608

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C132H205N29O40S

Absent amino acids  ACFGHNPQRSV

Common amino acids  E

Mass  2870.31

Pl  4.82

Basic residues  5

Acidic residues  7

Hydrophobic residues  6

Net charge  -2

Boman Index  -5592

Hydrophobicity  -133.18

Aliphatic Index  70.91

Half Life 

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

Extinction Coefficient cystines  12490

Absorbance 280nm  594.76

Polar residues  3



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