Enfuvirtide T-20

Names

[ Name ]:
Enfuvirtide T-20

[Synonym ]:
T-20
Enfuvirtide Acetate (T-20)
enfuvirtide
UNII-19OWO1T3ZE
Fuzeon
DP178
acetyl-L-tyrosyl-L-threonyl-L-seryl-L-leucyl-L-isoleucyl-L-histidyl-L-seryl-L-leucyl-L-isoleucyl-L-a-glutamyl-L-a-glutamyl-L-seryl-L-glutaminyl-L-asparaginyl-L-glutaminyl-L-glutaminyl-L-a-glutamyl-L-lysyl-L-asparaginyl-L-a-glutamyl-L-glutaminyl-L-a-glutamyl-L-leucyl-L-leucyl-L-a-glutamyl-L-leucyl-L-a-aspartyl-L-lysyl-L-tryptophyl-L-alanyl-L-seryl-L-leucyl-L-tryptophyl-L-asparaginyl-L-tryptophyl-L-phenylalaninamide
Pentafuside
T 20 (peptide)
Enfuvirtide Acetate

Biological Activity

[Description]:

Enfuvirtide is an anti-HIV-1 fusion inhibitor peptide. Sequence: Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2.

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV

Peptides

Research Areas >> Infection

[Target]

HIV fusion[1]

[In Vitro]

A cell-cell fusion assay reveals that the effective concentration for achieving 50% inhibition (IC50) of Enfuvirtide is 23 ± 6 nM[2]. IFN-λs (1, 2, or 3) or the antiretrovirals (AZT, Efavirenz, Indinavir, and Enfuvirtide) significantly inhibita the expression of HIV p24 antigen and Gag gene in macrophages. IFN-λs (1, 2, or 3) also enhanced the anti-HIV (Bal) effect of AZT, Efavirenz, Indinavir, and Enfuvirtide[3].

[In Vivo]

Enfuvirtide has a T1/2 of 3.8 h[2].

[Animal admin]

For infection with the resistant HIV strains, 7-day-cultured macrophages (105 cells/well in 96-well plates) are incubated with or without IFN-λ1, λ2, or λ3 (100 ng/mL each) and/or anti-HIV drugs: Azidothymidine (AZT) 10 pM; Efavirenz 100 pM; Indinavir 10-3 pM, and Enfuvirtide 10 nM for 24 h. Cells are then infected with different strains of HIV (6 ng p24/well) for 2 h. After washed three times with plain DMEM, cells are cultured with fresh 10% DMEM containing IFN-λs and/or antiretroviral drugs. For HIV Bal infection, culture supernatant is harvested at day 8 post infection for RT and p24 assays. Infected and untreated cells served as controls. HIV Gag gene expression in infected cells is also examined at day 8 post infection. For anti-HIV drug-resistant virus (A012 G691-6 or TC49) infection, culture supernatant is harvested for HIV p24 protein by ELISA at days 3, 5, 7, and 10 postinfection. The cell cultures are replaced with the fresh media supplemented with IFN-λ1, λ2, or λ3 and/or the antiretrovirals every 2–3 days. The culture supernatant collected at day 10 postinfection is also subjected to RT assay[3].

[References]

[1]. Figueira TN, et al. Quantitative analysis of molecular partition towards lipid membranes using surface plasmon resonance. Sci Rep. 2017 Mar 30;7:45647.

[2]. Cao P, et al. The improved efficacy of Sifuvirtide compared with Enfuvirtide might be related to its selectivity for the rigid biomembrane, as determined through surface plasmon resonance. PLoS One. 2017 Feb 16;12(2):e0171567.

[3]. Wang X, et al. IFN-λ Inhibits Drug-Resistant HIV Infection of Macrophages. Front Immunol. 2017 Mar 6;8:210.

[Related Small Molecules]