DRAVP ID  DRAVPe00647

Peptide Name   ENF (T-20)

Sequence  YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF

Sequence Length  36

UniProt ID  P04578 

Source  Synthetic construct

Target Organism  HIV,SIV

Assay  MAGI/cMAGI infectivity assay,neutralization assay

Activity 

• [Ref.17640899]HIV IIIB:inhibition of virus infection on CEM4 cells(IC50=0.006 μg/ml);
• HIV 098:inhibition of virus infection on CEM4 cells(IC50=0.050 μg/ml);
• HIV 098-T20:inhibition of virus infection on CEM4 cells(IC50=0.526 μg/ml);
• HIV 098-T1249:inhibition of virus infection on CEM4 cells(IC50=54.958 μg/ml);
• HIV 098-T651:inhibition of virus infection on CEM4 cells(IC50=47.822 μg/ml).
• [Ref.31228294]HIV-1 N43:inhibition of virus infection in U87 cells(IC50=0.37 µg/ml);
• HIV-1 JRCSF:inhibition of virus infection in U87 cells(IC50=0.09 µg/ml);
• HIV-1 94UG103:inhibition of pseudovirus infection in U87 cells(IC50=0.03 µg/ml);
• HIV-1 92BR020:inhibition of pseudovirus infection in U87 cells(IC50=0.30 µg/ml);
• HIV-1 IAVI C22:inhibition of pseudovirus infection in U87 cells(IC50=0.03 µg/ml);
• HIV-1 92HT021:inhibition of pseudovirus infection in U87 cells(IC50=0.02 µg/ml);
• HIV-1 JRCSF-GIA:inhibition of pseudovirus infection in U87 cells(IC50=3.58 µg/ml).
• [Ref.30089693]HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=24633±2467 pM);
• HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=10825±1354 pM);
• HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=4503±384 pM);
• HIV-1(3 A, 13 B, 7 C, 1 G, 1 A/C, 5 A/E, 6 B/C pseudovirus subtypes):inhibition of pseudovirus infection in TZM-bl cells(IC50=34858 pM);
• T-20 sensitive HIV-1(NL4-3D36G):inhibition of virus infection in TZM-bl cells(IC50=9.12 nM);
• T-20 resistant HIV-1 NL4-3(WT,I37T,V38A,V38 M,Q40H,N43K,G36S/V38 M,I37T/N43K,V38A/N42T):inhibition of virus infection in TZM-bl cells(IC50=90.18-2250 nM);
• HIV-2(ROD,ST):inhibition of virus infection in TZM-bl cells(IC50=263.68-829.01 nM);
• SIV(239,PBJ):inhibition of virus infection in TZM-bl cells(IC50=490.8-648.49 nM).

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

Cytotoxicity 

• [Ref.30089693]TZM-bl cell:CC50=157.87 ± 8.79 μM;
• MT-4 cell:CC50=171.73± 23.13 μM;
• HEK293T cell:CC50=216.23± 33.08 μM;
• PBMC:CC50=81.23± 4.59 μM.

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.

PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L

Literature 1

Title   Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.

Pubmed ID   17640899

Reference   Proc Natl Acad Sci U S A. 2007 Jul 31;104(31):12772-7. 

Author   Dwyer JJ, Wilson KL, Davison DK, Freel SA, Seedorff JE, Wring SA, Tvermoes NA, Matthews TJ, Greenberg ML, Delmedico MK.

DOI   10.1073/pnas.0701478104

Literature 2

Title   Optimization of peptidic HIV-1 fusion inhibitor T20 by phage display.

Pubmed ID   31228294

Reference   Protein Sci. 2019 Aug;28(8):1501-1512.

Author   Chen G, Cook JD, Ye W, Lee JE, Sidhu SS.

DOI   10.1002/pro.3669

Literature 3

Title   Structural and Functional Characterization of Membrane Fusion Inhibitors with Extremely Potent Activity against Human Immunodeficiency Virus Type 1 (HIV-1), HIV-2, and Simian Immunodeficiency Virus.

Pubmed ID   30089693

Reference   J Virol. 2018 Sep 26;92(20):e01088-18.

Author   Chong H, Zhu Y, Yu D, He Y.

DOI   10.1128/JVI.01088-18