[HTML][HTML] PET agents in dementia: an overview

A van Waarde, S Marcolini, PP De Deyn… - Seminars in nuclear …, 2021 - Elsevier
This article presents an overview of imaging agents for PET that have been applied for
research and diagnostic purposes in patients affected by dementia. Classified by the target …

Recent developments in carbon-11 chemistry and applications for first-in-human PET studies

A Pees, M Chassé, A Lindberg, N Vasdev - Molecules, 2023 - mdpi.com
Positron emission tomography (PET) is a molecular imaging technique that makes use of
radiolabelled molecules for in vivo evaluation. Carbon-11 is a frequently used radionuclide …

Insights into current tropomyosin receptor kinase (TRK) inhibitors: development and clinical application

W Yan, NR Lakkaniga, F Carlomagno… - Journal of medicinal …, 2018 - ACS Publications
The use of kinase-directed precision medicine has been heavily pursued since the
discovery and development of imatinib. Annually, it is estimated that around∼ 20 000 new …

Structural Optimization and Structure–Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New …

S Pan, L Zhang, X Luo, J Nan, W Yang… - Journal of Medicinal …, 2022 - ACS Publications
Tropomyosin receptor kinases (TrkA, TrkB, and TrkC) are attractive therapeutic targets for
multiple cancers. Two first-generation small-molecule Trks inhibitors, larotrectinib and …

Automated synthesis of PET radiotracers by copper‐mediated 18F‐fluorination of organoborons: Importance of the order of addition and competing protodeborylation

AV Mossine, AF Brooks… - Journal of Labelled …, 2018 - Wiley Online Library
In this paper, we describe the use of Cu‐mediated [18F] fluorodeboronation for the
automated production of positron emission tomography radiotracers suitable for clinical use …

Discovery of 3-pyrazolyl-substituted pyrazolo [1, 5-a] pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance

Y Gong, FX Wu, MS Wang, HC Xu, LS Zhuo… - European Journal of …, 2022 - Elsevier
Several secondary tropomyosin receptor kinase (TRK) mutations located in the solvent front,
xDFG, and gatekeeper regions, are a common cause of clinical resistance. Mutations in the …

Design, synthesis, and Structure–Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors

Y Duan, J Wang, S Zhu, ZC Tu, Z Zhang, S Chan… - European Journal of …, 2020 - Elsevier
Neurotrophic receptor tyrosine kinase (NTRK) fusions are oncogenic drivers for a variety of
adult and pediatric tumors, validated by the US FDA approval of small molecular Trk …

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

V Bernard-Gauthier, AV Mossine… - 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 …

Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors

Q Qin, Q Fu, X Wang, R Lv, S Lu, Z Guo, T Wu… - European Journal of …, 2023 - Elsevier
Tropomyosin receptor kinases (TRKs) are effective targets for anti-cancer drug discovery.
The first-generation type I TRKs inhibitors, larotrectinib and entrectinib, exhibit durable …

First-in-Human Brain Imaging of [18F]TRACK, a PET tracer for Tropomyosin Receptor Kinases

JJ Bailey, L Kaiser, S Lindner, M Wüst… - ACS chemical …, 2019 - ACS Publications
The tropomyosin receptor kinase TrkA/B/C family is responsible for human neuronal growth,
survival, and differentiation from early nervous system development stages onward …