We also review the differences between the seven NOX family members in terms of structure and function in health and disease and then focus on the most advanced NOX inhibitors with an …

In this review, we will provide an updated overview of the available Nox inhibitors, both peptidic and small molecules, and discuss the body of data related to their possible mechanisms of …

Novel NOX inhibitors stemming from rational drug discovery approaches, for example, GKT137831, ML171, and VAS2870, show improved specificity for NADPH oxidases and …

Recently, Jaquet et al. tested celastrol on various NOX isoforms, and found that it acts as a general NOX inhibitor with some selectivity for NOX1 and NOX2 (IC 50 values of 0.4 and 0.6 …

To date, identification of selective NOX inhibitors is quite challenging, precluding a pharmacologic demonstration of NOX as therapeutic targets in vivo. The aim of this Perspective is to furnish …

Jun 7, 2021 · In this study we have developed a new specific small molecule Nox2/Nox4 inhibitor (GLX481304), and show, using isolated cardiomyocytes and perfused whole hearts from …

May 1, 2020 · VAS2870 and VAS3947 are covalent bona-fide NOX inhibitors. A conserved active-site cysteine can be targeted for inhibition. NADPH-oxidases (NOXs) purposefully produce …

Oct 26, 2023 · Here, we describe fully validated human NOX inhibitors, obtained from an in silico screen, targeting the active site of Cylindrospermum stagnale NOX5 (csNOX5).

Clinical trials in patients with GKT137831 have demonstrated excellent tolerability and reduction of various markers of chronic inflammation. NOX1/4 inhibition may provide a safe and effective …

Sep 9, 2013 · An ideal Nox inhibitor would not inhibit other sources of ROS such as xanthine oxidase, would be devoid of ROS-scavenging or cytotoxic properties, would efficaciously and …