Related Experiment Video

Updated: Sep 13, 2025

Fluorescent Leakage Assay to Investigate Membrane Destabilization by Cell-Penetrating Peptide
07:33

Fluorescent Leakage Assay to Investigate Membrane Destabilization by Cell-Penetrating Peptide

Published on: December 19, 2020

6.5K

A Short Peptide Inhibitor of Measles Virus Fusion Protein that Exhibits Passive Membrane Permeability

Ziwei Gao1, Jiei Sasaki2, Tateki Suzuki2

  • 1Department of Chemistry & Biotechnology, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-8656, Japan.

Chemmedchem
|July 28, 2025
PubMed

Insights

Researchers developed a new measles virus fusion protein (MeV-F) inhibitor. This peptide shows improved activity and membrane permeability, offering potential for orally available measles antiviral drugs.

Area of Science:

  • Virology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Measles virus (MeV) is highly contagious with no approved antiviral treatments.
  • The measles virus fusion protein (MeV-F) is essential for viral entry and a key drug target.
  • Existing fusion inhibitor peptides (FIPs) require enhanced activity and membrane permeability for oral drug development.

Purpose of the Study:

  • To design and synthesize novel MeV-F inhibitors with improved oral bioavailability.
  • To enhance both the inhibitory potency and passive membrane permeability of FIPs.

Main Methods:

  • Chemical modification of FIPs using hydrogen-to-fluorine substitution.
  • Evaluation of inhibitory activity (IC50) and passive membrane permeability (Pe) of FIP derivatives.

Main Results:

  • Identified a novel FIP derivative with significantly enhanced inhibitory activity (IC50 = 90 nM).
  • Achieved improved passive membrane permeability (Pe = 1.4 × 10^-6 cm/s) in the FIP derivative.
  • Demonstrated the potential of modified FIPs as orally available MeV-F inhibitors.

Conclusions:

  • The developed FIP derivative represents a promising lead compound for oral measles antiviral therapy.
  • Hydrogen-to-fluorine substitution is an effective strategy for optimizing FIP properties.
  • Further development of these FIP derivatives could lead to the first orally available measles treatment.
Keywords:
fluorinationfusion inhibitor peptidesmeasles virusmembrane permeability

More Related Videos

Peptide Scanning-assisted Identification of a Monoclonal Antibody-recognized Linear B-cell Epitope08:09

Peptide Scanning-assisted Identification of a Monoclonal Antibody-recognized Linear B-cell Epitope

Published on: March 24, 2017

9.6K
A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation07:53

A Fluorogenic Peptide Cleavage Assay to Screen for Proteolytic Activity: Applications for coronavirus spike protein activation

Published on: January 9, 2019

33.3K

Related Concept Videos

Protein Diffusion in the Membrane01:24

Protein Diffusion in the Membrane

Proteins show rotational as well as lateral diffusion across the membrane. The lateral diffusion of proteins was confirmed through the cell fusion experiment where mouse and human cells were fused, resulting in hybrid cells. When the human and mouse cells fused, the specific membrane proteins on human and mouse cells were marked with the red and green-fluorescent markers, respectively. Initially, the red and green fluorescence was located on the respective hemisphere of the cell. As time...
4.6K
Single-pass Transmembrane Proteins01:25

Single-pass Transmembrane Proteins

Integral membrane proteins are tightly associated with the cell membrane and play a crucial role in cell communication, signaling, adhesion, and transport of the molecules. Some integral membrane proteins are present only in the membrane monolayer. For example, the enzyme fatty acid amide hydrolase is present in the cytoplasmic side of the membrane monolayer. In contrast, another type of integral membrane protein, also known as a transmembrane protein, spans across the membrane. Transmembrane...
5.3K
Membrane Fluidity01:23

Membrane Fluidity

Cell membranes are composed of phospholipids, proteins, and carbohydrates loosely attached to one another through chemical interactions. Molecules are generally able to move about in the plane of the membrane, giving the membrane its flexible nature called fluidity. Two other features of the membrane contribute to membrane fluidity: the chemical structure of the phospholipids and the presence of cholesterol in the membrane.
156.5K