General Information


DRAVP ID  DRAVPe00245

Peptide Name   T-20S[138E]

Sequence  YTSLIHSLIEEEQNQQEKNEQELLELDKWASLWNWF

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=283± 80 nM);
  • HIV-1V38A:inhibition of virus replication in HeLa cells(EC50>1000 nM);
  • HIV-1N43D:inhibition of virus replication in HeLa cells(EC50>1000 nM);
  • HIV-1N43D/S138A:inhibition of virus replication in HeLa cells(EC50>1000 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  DRAVPe00245

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  None

Stereochemistry  L



Physicochemical Information


Formula  C204H300N50O65

Absent amino acids  CGMPRV

Common amino acids  E

Mass  4492.92

Pl  4.21

Basic residues  3

Acidic residues  8

Hydrophobic residues  13

Net charge  -5

Boman Index  -7600

Hydrophobicity  -95

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  8



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