General Information


DRAVP ID  DRAVPe01769

Peptide Name   CMK

Sequence  RVKR

Sequence Length  4

UniProt ID  No entry found

Source  Synthetic construct



Activity Information


Target Organism  SARS-CoV-2

Assay  Plaque assay

Activity 

  • [Ref.33007239]SARS-CoV-2:inhibition of virus production in Vero E6 cells(IC50=0.057 µM).
  • [Ref.31683742]Virus:Zika virus (ZIKV):inhibition of virus release in Vero cells(IC50=18.59 µM);Japanese encephalitis virus (JEV):inhibition of virus release in BHK-21 cells(IC50=19.91 µM).
  • [Ref.23617302]Hepatitis B virus (HBV):Inhibition of HBeAg secretion in HepG2.2.15 cells(26±11% inhibition at 20 µM,21±13% Inhibition at 100 µM).

Hemolytic Activity  No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity 

  • [Ref.31683742]Vero cells:CC50=712.9 µM.
  • [Ref.33007239]Vero E6 cells:IC50=318.2 µM.

Binding Target  Not found

Mechanism  CMK blocks virus entry, but it further suppresses cleavage of spikes and the syncytium.



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Decanoyl(C10)

C-terminal Modification  chloromethylketone(CMK)

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C23H47N11O5

Absent amino acids  ACDEFGHILMNPQSTWY

Common amino acids  R

Mass  557.7

Pl  12.01

Basic residues  3

Acidic residues  0

Hydrophobic residues  1

Net charge  3

Boman Index  -3135

Hydrophobicity  -217.5

Aliphatic Index  72.5

Half Life 

  •     Mammalian:1 hour
  •     Yeast:2 min
  •     E.coli:2 min

Extinction Coefficient cystines  0

Absorbance 280nm  0

Polar residues  0



Literature Information


Literature 1

Title   Therapeutic potential of furin inhibitors for the chronic infection of hepatitis B virus.

Pubmed ID   23617302

Reference   Liver Int. 2013 Sep;33(8):1230-8.

Author   Pang YJ, Tan XJ, Li DM, Zheng ZH, Lei RX, Peng XM.

DOI   10.1111/liv.12185

Literature 2

Title   Decanoyl-Arg-Val-Lys-Arg-Chloromethylketone: An Antiviral Compound That Acts against Flaviviruses through the Inhibition of Furin-Mediated prM Cleavage.

Pubmed ID   31683742

Reference   Viruses. 2019 Oct 31;11(11):1011.

Author   Imran M, Saleemi MK, Chen Z, Wang X, Zhou D, Li Y, Zhao Z, Zheng B, Li Q, Cao S, Ye J.

DOI   10.3390/v11111011

Literature 3

Title   Furin Inhibitors Block SARS-CoV-2 Spike Protein Cleavage to Suppress Virus Production and Cytopathic Effects.

Pubmed ID   33007239

Reference   Cell Rep. 2020 Oct 13;33(2):108254.

Author   Cheng YW, Chao TL, Li CL, Chiu MF, Kao HC, Wang SH, Pang YH, Lin CH, Tsai YM, Lee WH, Tao MH, Ho TC, Wu PY, Jang LT, Chen PJ, Chang SY, Yeh SH.

DOI   10.1016/j.celrep.2020.108254