Related Experiment Video

Updated: Jun 10, 2026

Simultaneous Measurement of Superoxide/Hydrogen Peroxide and NADH Production by Flavin-containing Mitochondrial Dehydrogenases
08:57

Simultaneous Measurement of Superoxide/Hydrogen Peroxide and NADH Production by Flavin-containing Mitochondrial Dehydrogenases

Published on: February 24, 2018

Small-molecule inhibitors of NADPH oxidase 4

Gábor Borbély1, István Szabadkai, Zoltán Horváth

  • 1Vichem Chemie Research Ltd., Budapest, Hungary. gabor.borbely@kkk.org.hu

Journal of Medicinal Chemistry
|August 25, 2010
PubMed

Insights

Researchers discovered novel inhibitors for NADPH oxidase 4 (NOX4), an enzyme implicated in oxidative stress diseases. This development addresses the lack of specific NOX inhibitors, offering potential therapeutic avenues.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • NADPH oxidase (NOX) enzymes are key players in oxidative damage and related diseases.
  • Currently, no specific inhibitors targeting NOX enzymes are available for therapeutic use.

Purpose of the Study:

  • To discover and develop novel inhibitors specifically targeting NOX4.

Main Methods:

  • Utilized compound libraries for a primary screen using a cell-based assay.
  • Monitored hydrogen peroxide (H2O2) production to assess NOX4 activity inhibition.

Main Results:

  • Identified twenty-four compounds that inhibited NOX4 activity.
  • These compounds demonstrated low-micromolar IC50 values.
  • Three promising compounds were selected for further drug development.

Conclusions:

  • Successfully discovered novel NOX4 inhibitors.
  • These findings represent a significant step towards developing specific NOX inhibitors for treating oxidative damage-related diseases.

More Related Videos

Bioluminescence Imaging of NADPH Oxidase Activity in Different Animal Models10:42

Bioluminescence Imaging of NADPH Oxidase Activity in Different Animal Models

Published on: October 22, 2012

A Semi-High-Throughput Adaptation of the NADH-Coupled ATPase Assay for Screening Small Molecule Inhibitors10:28

A Semi-High-Throughput Adaptation of the NADH-Coupled ATPase Assay for Screening Small Molecule Inhibitors

Published on: August 17, 2019

Related Concept Videos

The Electron Transport Chain01:30

The Electron Transport Chain

The electron transport chain or oxidative phosphorylation is an exothermic process in which free energy released during electron transfer reactions is coupled to ATP synthesis. This process is a significant source of energy in aerobic cells, and therefore inhibitors of the electron transport chain can be detrimental to the cell's metabolic processes.
Inhibitors of the electron transport chain
Rotenone, a widely used pesticide, prevents electron transfer from Fe-S cluster to ubiquinone or Q in...
Role of Reduced Coenzymes NADH and FADH₂01:29

Role of Reduced Coenzymes NADH and FADH₂

The energy released from the breakdown of the chemical bonds within nutrients can be stored either through the reduction of electron carriers or in the bonds of adenosine triphosphate (ATP). In living systems, a small class of compounds functions as mobile electron carriers, molecules that bind to and shuttle high-energy electrons between compounds in pathways. The principal electron carriers that will be considered originate from the B vitamin group and are derivatives of nucleotides; they are...
Electron Transport Chain: Complex III and IV01:43

Electron Transport Chain: Complex III and IV

During the electron transport chain, electrons from NADH and FADH2 are first transferred to complexes I and II, respectively. These two complexes then transfer the electrons to ubiquinol, which carries them further to complex III. Complex III passes the electrons across the intermembrane space to Cyt c, which carries them further to complex IV. Complex IV donates electrons to oxygen and reduces it to water. As electrons pass through complexes I, III, and IV, the energy released aids the pumping...
Oxidation of Phenols to Quinones01:17

Oxidation of Phenols to Quinones

In the presence of oxidizing agents, phenols are oxidized to quinones. Quinones can be easily reduced back to phenols using mild reducing agents. The electron-donating hydroxyl group enhances the reactivity of the aromatic ring, enabling oxidation of the ring even in the absence of an α hydrogen.
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox property is crucial in...
Oxidation and Reduction of Organic Molecules01:19

Oxidation and Reduction of Organic Molecules

Energy production within a cell involves many coordinated chemical pathways. Most of these pathways are combinations of oxidation and reduction reactions, which occur at the same time. An oxidation reaction strips an electron from an atom in a compound, and the addition of this electron to another compound is a reduction reaction. Because oxidation and reduction usually occur together, these pairs of reactions are called redox reactions.
The removal of an electron from a molecule, results in a...
Antiprotozoal Agents01:21

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...