Toward Novel [¹⁸F]Fluorine-Labeled Radiotracers for the Imaging of α-Synuclein Fibrils.

ABSTRACT: The accumulation of α-synuclein aggregates (α-syn) in the human brain is an occurrence common to all α-synucleinopathies. Non-invasive detection of these aggregates in a living brain with a target-specific radiotracer is not yet possible. We have recently discovered that the inclusion of a methylenedioxy group in the structure of diarylbisthiazole (DABTA)-based tracers improves binding affinity and selectivity to α-syn. Subsequently, complementary in silico modeling and machine learning (ML) of tracer-protein interactions were employed to predict surface sites and structure-property relations for the binding of the ligands. Based on this observation, we developed a small focused library of DABTAs from which 4-(benzo[d][1,3]dioxol-5-yl)-4'-(3-[¹⁸F]fluoro-4-methoxyphenyl)-2

SUBMITTER: Uzuegbunam BC 

PROVIDER: S-EPMC9099256 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature