BACE1: Now We Can See You.

Authors :: Bongarzone S
Gee AD
Source :: Journal of medicinal chemistry [J Med Chem] 2018 Apr 26; Vol. 61 (8), pp. 3293-3295. Date of Electronic Publication: 2018 Apr 04.
Publication Year :: 2018
Abstract: No in vivo imaging biomarker currently exists for BACE, a drug target for Alzheimer's disease (AD). A strategy aiming to find a novel brain-penetrant positron emission tomography (PET) radiotracer for BACE1 led to the discovery of a highly potent and selective aminothiazine inhibitor, PF-06684511. This scaffold has been now evaluated as BACE1 PET radiotracer ([ <superscript>18</superscript> F]PF-06684511) after labeling with fluorine-18 ( <superscript>18</superscript> F), allowing its evaluation in non-human primates (NHP) as the first a brain-penetrant PET radiotracer for imaging BACE1 in vivo.