Copper-Mediated Radiocyanation of Unprotected Amino Acids and Peptides

…, M Horikawa, X Shao, WP Winton, J Stauff… - Journal of the …, 2022 - ACS Publications
This report describes a copper-mediated radiocyanation of aryl halides that is applicable to
complex molecules. This transformation tolerates an exceptionally wide range of functional …

Structural basis for achieving GSK-3β inhibition with high potency, selectivity, and brain exposure for positron emission tomography imaging and drug discovery

…, SA Reis, JM Chen, X Shao, J Stauff… - Journal of medicinal …, 2019 - ACS Publications
Using structure-guided design, several cell based assays, and microdosed positron emission
tomography (PET) imaging, we identified a series of highly potent, selective, and brain-…

Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging

…, A Aliaga, JJ Bailey, X Shao, J Stauff… - Journal of Medicinal …, 2018 - ACS Publications
Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic
Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the …

[HTML][HTML] Synthesis and Initial In Vivo Evaluation of [11C]AZ683—A Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R)

SS Tanzey, X Shao, J Stauff, J Arteaga, P Sherman… - Pharmaceuticals, 2018 - mdpi.com
Positron emission tomography (PET) imaging of Colony Stimulating Factor 1 Receptor (CSF1R)
is a new strategy for quantifying both neuroinflammation and inflammation in the …

Synthesis and evaluation of NLRP3-inhibitory sulfonylurea [11C] MCC950 in healthy animals

JR Hill, X Shao, NL Massey, J Stauff… - Bioorganic & medicinal …, 2020 - Elsevier
The diaryl sulfonylurea MCC950/CRID3 is a potent NLRP3 inhibitor (IC 50 = 8 nM) and, in
animal models, MCC950 protects against numerous NLRP3-related neurodegenerative …

[HTML][HTML] Synthesis and evaluation of a fluorine-18 radioligand for imaging Huntingtin aggregates by positron emission tomographic imaging

…, AF Brooks, A Lapsys, TJ Desmond, J Stauff… - Frontiers in …, 2021 - frontiersin.org
Mutations in the huntingtin gene (HTT) triggers aggregation of huntingtin protein (mHTT),
which is the hallmark pathology of neurodegenerative Huntington’s disease (HD). …

Zinc‐Mediated Radiosynthesis of Unprotected Fluorine‐18 Labelled α‐Tertiary Amides

…, R Ma, EW Webb, WP Winton, J Stauff… - Angewandte Chemie …, 2024 - Wiley Online Library
This report describes the development of a Zn(OTf) 2 ‐mediated method for converting α‐tertiary
haloamides to the corresponding fluorine‐18 labelled α‐tertiary fluoroamides with no‐…

[HTML][HTML] Strategies for PET imaging of the receptor for advanced glycation endproducts (RAGE)

LR Drake, AF Brooks, J Stauff, PS Sherman… - Journal of …, 2020 - Elsevier
The implication of the receptor for advanced glycation end-products (RAGE) in numerous
diseases and neurodegenerative disorders makes it interesting both as a therapeutic target …

Automated production of [11C] butyrate for keto body PET imaging

…, DM Raffel, RA Koeppe, WP Winton, J Stauff… - Nuclear medicine and …, 2023 - Elsevier
The report describes an updated, fully automated method for the production of [ 11 C]butyrate,
validated for use in clinical studies. A commercially available GE Tracerlab FX M synthesis …

Evaluating immunotherapeutic outcomes in triple negative breast cancer with a cholesterol radiotracer in mice

NG Ciavattone, JN Guan, A Farfel, J Stauff… - JCI …, 2024 - Am Soc Clin Investig
Evaluating the response to immune checkpoint inhibitors (ICIs) remains an unmet challenge
in 25 triple-negative breast cancer (TNBC). The requirement of cholesterol for activation and …