General Information

General Information

DRAVP ID DRAVPe00520

Peptide Name T-20(Enfuvirtide)

Sequence YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF

Sequence Length 36

UniProt ID No entry found

Source Synthetic construct

Other Link DRAVPa0326

Activity Information

Target Organism HIV

Assay MAGI/cMAGI infectivity assay,neutralization assay

Activity

[Ref.19073606]HIV-1WT:inhibition of virus replication in HeLa cells(EC50=2.4 ± 0.6 nM);
HIV-1V38A:inhibition of virus replication in HeLa cells(EC50=23± 8.2 nM);
HIV-1N43D:inhibition of virus replication in HeLa cells(EC50=49 ± 10 nM);
HIV-1N43D/S138A:inhibition of virus replication in HeLa cells(EC50=84 ± 16 nM).
[Ref.27795416]HIV-1 IIIB:inhibition of virus infection in MT-2 cells(IC50=71.8±2.2 nM); inhibition of peptide against cell-cell fusion between H9/HIV-1 IIIB cells and MT-2 cells(IC50=91.0± 1.2 nM);
HIV-1 Bal:inhibition of virus infection in MT-2 cells(IC50=70.5 ±0.9 nM);
HIV-1 clinical isolates(8 clinical isolates):inhibition of virus infection in MT-2 cells(IC50=20.4-157.3 nM);
HIV-1 pseudoviruses(7 pseudoviruses):inhibition of pseudoviruses infection in MT-2 cells(IC50=7.1-91.0 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 acts by binding to the heptad repeat 1 (HR1) region of gp41 and preventing the interaction of the HR1 and HR2 domains, which is required for virus–cell fusion.

Structure Information

PDB ID None

Predicted Structure Download DRAVPe00520

Linear/Cyclic Linear

N-terminal Modification Free

C-terminal Modification Free

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C202H298N50O64

Absent amino acids CGMPRV

Common amino acids EL

Mass 4450.88

Pl 4.3

Basic residues 3

Acidic residues 7

Hydrophobic residues 13

Net charge -4

Boman Index -7259

Hydrophobicity -87.5

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

Literature 2

Title Creating an Artificial Tail Anchor as a Novel Strategy To Enhance the Potency of Peptide-Based HIV Fusion Inhibitors.

Pubmed ID 27795416

Reference J Virol. 2016 Dec 16;91(1):e01445-16.

Author Su S, Zhu Y, Ye S, Qi Q, Xia S, Ma Z, Yu F, Wang Q, Zhang R, Jiang S, Lu L.

DOI 10.1128/JVI.01445-16