General Information


DRAVP ID  DRAVPe00231

Peptide Name   T-20S[138G]

Sequence  YTSLIHSLIEEGQNQQEKNEQELLELDKWASLWNWF

Sequence Length  36

UniProt ID  No entry found

Source  Synthetic construct(derived from Enfuvirtide)



Activity Information


Target Organism  HIV

Assay  MAGI assay

Activity 

  • [Ref.19073606]HIV-1WT:inhibition of virus replication in HeLa cells(EC50=1.3± 0.5 nM);
  • HIV-1V38A:inhibition of virus replication in HeLa cells(EC50=65± 8.8 nM);
  • HIV-1N43D:inhibition of virus replication in HeLa cells(EC50=141±26 nM);
  • HIV-1N43D/S138A:inhibition of virus replication in HeLa cells(EC50=185±68 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 prevents interactions between the C-HR and the N-terminal HR (N-HR) of gp41, thus interfering with conformational changes that are required for viral fusion.



Structure Information


PDB ID  None

Predicted Structure Download  DRAVPe00231

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C201H296N50O63

Absent amino acids  CMPRV

Common amino acids  EL

Mass  4420.86

Pl  4.3

Basic residues  3

Acidic residues  7

Hydrophobic residues  13

Net charge  -4

Boman Index  -6825

Hydrophobicity  -86.39

Aliphatic Index  89.44

Half Life 

  •     Mammalian:2.8 hour
  •     Yeast:10 min
  •     E.coli:2 min

Extinction Coefficient cystines  17990

Absorbance 280nm  514

Polar residues  9



Literature Information


Literature 1

Title   Design of peptide-based inhibitors for human immunodeficiency virus type 1 strains resistant to T-20.

Pubmed ID   19073606

Reference   J Biol Chem. 2009 Feb 20;284(8):4914-20.

Author   Izumi K, Kodama E, Shimura K, Sakagami Y, Watanabe K, Ito S, Watabe T, Terakawa Y, Nishikawa H, Sarafianos SG, Kitaura K, Oishi S, Fujii N, Matsuoka M.

DOI   10.1074/jbc.M807169200