BACE1: Now We Can See You

Salvatore Bongarzone; Antony D Gee

doi:10.1021/acs.jmedchem.8b00474

BACE1: Now We Can See You

Salvatore Bongarzone, Antony D Gee

School of Biomedical Engineering & Imaging Sciences, 4th Floor Lambeth Wing , St Thomas' Hospital, King's College London , London SE1 7EH , United Kingdom.

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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 ([18F]PF-06684511) after labeling with fluorine-18 (18F), allowing its evaluation in non-human primates (NHP) as the first a brain-penetrant PET radiotracer for imaging BACE1 in vivo.

Original language	English
Pages (from-to)	3293-3295
Number of pages	3
Journal	Journal of Medicinal Chemistry
DOIs	https://doi.org/10.1021/acs.jmedchem.8b00474
Publication status	Published - 4 Apr 2018

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BACE1 Now we can_BONGARZONE_Publishedonline4April2018_GREEN AAMAccepted author manuscript, 656 KB

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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 ([18F]PF-06684511) after labeling with fluorine-18 (18F), allowing its evaluation in non-human primates (NHP) as the first a brain-penetrant PET radiotracer for imaging BACE1 in vivo.",

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AB - 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 ([18F]PF-06684511) after labeling with fluorine-18 (18F), allowing its evaluation in non-human primates (NHP) as the first a brain-penetrant PET radiotracer for imaging BACE1 in vivo.

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BACE1: Now We Can See You

Abstract

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