The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis.

ABSTRACT: Essentials Signaling by Gas6 through Tyro3/Axl/Mer receptors is essential for stable platelet aggregation. UNC2025 is a small molecule inhibitor of the Mer tyrosine kinase. UNC2025 decreases platelet activation in vitro and thrombus formation in vivo. UNC2025's anti-platelet effect is synergistic with inhibition of the ADP receptor, P2Y₁₂ .

Summary

Background Growth arrest-specific protein 6 signals through the TAM (TYRO-3-AXL-MERTK) receptor family, mediating platelet activation and thrombus formation via activation of the aggregate-stabilizing α_IIb β₃ integrin. Objective To describe the antithrombotic effects mediated by UNC2025, a small-molecule MERTK tyrosine kinase inhibitor. Methods MERTK phosphorylation and downstream signaling were

SUBMITTER: Branchford BR 

PROVIDER: S-EPMC5858881 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature