Radiosynthesis of [¹⁸F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers.

ABSTRACT: Dihydroorotate dehydrogenase (DHODH), an enzyme that plays a critical role in the de novo pyrimidine biosynthesis, has been recognized as a promising target for the treatment of diseases that involve cellular proliferation, such as autoimmune diseases and cancers. Pharmacological inhibition of human DHODH (hDHODH) that offers a potential therapeutic strategy for the treatment in adult subjects with acute myeloid leukemia (AML) has recently been supported by phase I/II clinical trials for the treatment of patients with relapsed/refractory AML. To facilitate the development of optimized hDHODH inhibitors, the presence of an in vivo imaging probe that is able to demonstrate in vivo target engagement is critical and desirable. Brequinar is one of the most potent hDHODH inh

SUBMITTER: Banka VK 

PROVIDER: S-EPMC11320022 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature