Fluorinated pyrimidine 5-carboxamides as potential tools for MERTK targeted fluorine-18-PET-radioligand development.

ABSTRACT: MER tyrosine kinase (MERTK) is highly expressed on the protective and reparative phenotype of microglia, which is in response to neuroregeneration following the neuronal damage induced by multiple sclerosis (MS). A specific imaging tool, which can differentiate anti-inflammatory and immunosuppressive responses of microglia, could be highly beneficial for the early detection and clinical management of MS. To identify potential ¹⁸F-radiotracers to image anti-inflammatory responses of microglia, herein a series of fluorinated pyrimidine-5-carboxamide derivatives were prepared from a database of MERTK ligands. Several potent MERTK ligands were discovered with promising selectivity profiles over other off-targets (AXL, TYRO3 and FLT3). A cell-based assay was employed to assess cellul

SUBMITTER: Mudududdla R 

PROVIDER: S-EPMC12679506 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature