General Information


DRAVP ID  DRAVPe01847

Peptide Name   Entry 15

Sequence  GKRKSXAf

Sequence Length  8

UniProt ID  No entry found

Source  Synthetic construct



Activity Information


Target Organism  DENV

Assay  Fluorimetric assay

Activity 

  • [Ref.28539222]dengue virus 2(DENV2):inhibition of the activity of NS2B-NS3 protease(IC50= 7.6 μM).

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  NS2B-NS3 protease

Mechanism  The cyclic peptide could inhibit the activity of NS2B-NS3 protease, which is an essential enzyme for the replication of dengue virus.



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Cyclic

N-terminal Modification  No specific N-terminal

C-terminal Modification  No specific C-terminal

Other Modification  The 'X' at position 6 indicates homophenylalanine(hPhe). The N-terminal and C-terminal cyclized by a amide bond.

Stereochemistry  Mixed(D-Phe8)



Physicochemical Information


Formula  C26H47N11O6

Absent amino acids  CDEFHILMNPQTVWY

Common amino acids  K

Mass  904.27

Pl  11.17

Basic residues  3

Acidic residues  0

Hydrophobic residues  1

Net charge  3

Boman Index  -2667

Hydrophobicity  -146.25

Aliphatic Index  12.5

Half Life 

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

Extinction Coefficient cystines  0

Absorbance 280nm  0

Polar residues  2



Literature Information


Literature 1

Title   Discovery of novel cyclic peptide inhibitors of dengue virus NS2B-NS3 protease with antiviral activity.

Pubmed ID   28539222

Reference   Bioorg Med Chem Lett. 2017 Aug 1;27(15):3586-3590.

Author   Takagi Y, Matsui K, Nobori H, Maeda H, Sato A, Kurosu T, Orba Y, Sawa H, Hattori K, Higashino K, Numata Y, Yoshida Y.

DOI   10.1016/j.bmcl.2017.05.027