NADPH oxidase 2 inhibitor GSK2795039 exerts antiplatelet and antithrombotic activity.

ABSTRACT: Reactive oxygen species (ROS) production by NADPH oxidase (NOX) is a key promoter of platelet activation, making NOX inhibition an attractive antiplatelet strategy. This study evaluated the effects of the novel NOX2 inhibitor, GSK2795039, on human platelet functional responses and ROS-mediated signaling pathways. GSK2795039 effectively suppressed both extracellular and intracellular ROS production in collagen-stimulated platelets. Consequently, GSK2795039 treatment significantly inhibited collagen-induced platelet aggregation, dense-granule ATP release, and α-granule P-selectin exposure. Furthermore, GSK2795039 attenuated tyrosine phosphorylation-mediated activation of spleen tyrosine kinase (Syk), linker for the activation of T cells (LAT), vav guanine nucleotide exchange factor 1 (Vav1),

SUBMITTER: Oh EB 

PROVIDER: S-EPMC12533013 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature