[Enfuvirtide, mechanism of action and pharmacological properties].

Med Arh

Institu za farmakologiju, klinicku farmakologiju i toksikologiju, Univerziteta u Sarajevu.

Published: November 2005

Enfuvirtide is a new class of antiviral drug, fusion inhibitors, which interferate with penetration of HIV-1 in the cells. Enfuvirtide exhibits potent and selective inhibition of membrane of viral and cells. It specifically inhibits the function of the gp41 transmembrane glycoprotein of HIV-1. Enfurvitide showed significantly efficacy in the combination with other antiviral drugs in early stadium of HIV infection and in patients with antiretroviral resistention. Local injection site reactions are the most common adverse events associated with enfurvitide. However, the need for subcutaneous application of enfurvitide is a distinct disadvantage, especially in patients who are already burdened by complex oral therapy.

Download full-text PDF

Source

Publication Analysis

Top Keywords

[enfuvirtide mechanism
4
mechanism action
4
action pharmacological
4
pharmacological properties]
4
properties] enfuvirtide
4
enfuvirtide class
4
class antiviral
4
antiviral drug
4
drug fusion
4
fusion inhibitors
4

Similar Publications

Article Synopsis
  • Feline immunodeficiency virus (FIV) has structural similarities to human immunodeficiency virus (HIV), specifically in the glycoproteins that facilitate virus-host interactions.
  • The study focuses on a peptide sequence from FIV’s gp36, called gp36 NHR, which affects the antiviral effectiveness of another peptide, C8, derived from a different region of gp36.
  • Using techniques like CD, NMR, and molecular dynamics simulations, researchers found that gp36 NHR forms dynamic helix structures and may hinder the interaction between C8 and other crucial regions of the virus, providing insights for developing new antiviral strategies against FIV.
View Article and Find Full Text PDF
Article Synopsis
  • The six-helix bundle (6-HB) is crucial for the fusion of viruses with host membranes, and current peptide inhibitors like Enfuvirtide face issues such as drug resistance and short effectiveness.
  • This study focuses on creating new α-helical peptides as fusion inhibitors specifically targeting viruses like MERS-CoV and IAVs, using novel designs that are distinct from natural peptides.
  • The research identified an effective artificial C-peptide, named 1SR, which prevents HIV-1 fusion by disrupting the 6-HB formation, offering a promising lead for future antiviral developments.
View Article and Find Full Text PDF

Enfuvirtide was the first marketed fusion inhibitor that worked by binding to glycoprotein 41 of the HIV envelope, preventing the conformational changes required for HIV fusion with CD4+ T cells. Due to its novel mechanisms of action, it was frequently used in the past as part of regimens for the indication of multi-class-resistant HIV until newer oral agents emerged. Here, we describe the case of a 40-year-old man who used enfuvirtide injections from 2012 to 2017 inclusive for multi-class-resistant HIV until he presented in 2021 with an abscess overlying a right lower quadrant mass requiring drainage via pigtail.

View Article and Find Full Text PDF

Viral infection has become one of the worst human lethal diseases. In recent years, major gains have been made in the research of peptide-based antiviral agents on account of the mechanism of viral membrane fusion, among which the peptide Enfuvirtide has been listed for the treatment of AIDS. This paper reviewed a new way to design peptide-based antiviral agents by "bundling" superhelix with isopeptide bonds to construct the active advanced structure.

View Article and Find Full Text PDF

In our previous work, we replaced the TRM (tryptophan-rich motif) of T20 (Enfuvirtide) with fatty acid (C16) to obtain the novel lipopeptide LP-40, and LP-40 displayed enhanced antiviral activity. In this study, we investigated whether the C16 modification could enhance the high-resistance barrier of the inhibitor LP-40. To address this question, we performed an in vitro simultaneous screening of HIV-1 resistance to T20 and LP-40.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!