PET molecular imaging in drug development: the imaging and chemistry perspective
Positron emission tomography with selective radioligands advances the drug discovery and
development process by revealing information about target engagement, proof of …
development process by revealing information about target engagement, proof of …
[HTML][HTML] Potential applications for sigma receptor ligands in cancer diagnosis and therapy
A van Waarde, AA Rybczynska… - … et Biophysica Acta (BBA …, 2015 - Elsevier
Sigma receptors (sigma-1 and sigma-2) represent two independent classes of proteins.
Their endogenous ligands may include the hallucinogen N, N-dimethyltryptamine (DMT) …
Their endogenous ligands may include the hallucinogen N, N-dimethyltryptamine (DMT) …
Physiological blood–brain transport is impaired with age by a shift in transcytosis
The vascular interface of the brain, known as the blood–brain barrier (BBB), is understood to
maintain brain function in part via its low transcellular permeability,–. Yet, recent studies …
maintain brain function in part via its low transcellular permeability,–. Yet, recent studies …
Human umbilical cord plasma proteins revitalize hippocampal function in aged mice
JM Castellano, KI Mosher, RJ Abbey, AA McBride… - Nature, 2017 - nature.com
Ageing drives changes in neuronal and cognitive function, the decline of which is a major
feature of many neurological disorders. The hippocampus, a brain region subserving roles …
feature of many neurological disorders. The hippocampus, a brain region subserving roles …
The sigma-1 receptor modulates dopamine transporter conformation and cocaine binding and may thereby potentiate cocaine self-administration in rats
WC Hong, H Yano, T Hiranita, FT Chin… - Journal of Biological …, 2017 - ASBMB
The dopamine transporter (DAT) regulates dopamine (DA) neurotransmission by
recapturing DA into the presynaptic terminals and is a principal target of the psychostimulant …
recapturing DA into the presynaptic terminals and is a principal target of the psychostimulant …
Approaches to PET imaging of glioblastoma
LR Drake, AT Hillmer, Z Cai - Molecules, 2020 - mdpi.com
Glioblastoma multiforme (GBM) is the deadliest type of brain tumor, affecting approximately
three in 100,000 adults annually. Positron emission tomography (PET) imaging provides an …
three in 100,000 adults annually. Positron emission tomography (PET) imaging provides an …
Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one …
S Intagliata, A Sharma, TI King, C Mesangeau… - The AAPS Journal, 2020 - Springer
The sigma-2 receptor has been cloned and identified as Tmem97, which is a
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …
Knocking out sigma-1 receptors reveals diverse health problems
S Couly, N Goguadze, Y Yasui, Y Kimura… - Cellular and molecular …, 2020 - Springer
Abstract Sigma-1 receptor (Sig-1R) is a protein present in several organs such as brain,
lung, and heart. In a cell, Sig-1R is mainly located across the membranes of the …
lung, and heart. In a cell, Sig-1R is mainly located across the membranes of the …
[HTML][HTML] [18F] GE-180 PET detects reduced microglia activation after LM11A-31 therapy in a mouse model of Alzheimer's disease
ML James, NP Belichenko, AJ Shuhendler… - Theranostics, 2017 - ncbi.nlm.nih.gov
Microglial activation is a key pathological feature of Alzheimer's disease (AD). PET imaging
of translocator protein 18 kDa (TSPO) is a strategy to detect microglial activation in vivo …
of translocator protein 18 kDa (TSPO) is a strategy to detect microglial activation in vivo …
[HTML][HTML] Visualizing nerve injury in a neuropathic pain model with [18F] FTC-146 PET/MRI
The ability to locate nerve injury and ensuing neuroinflammation would have tremendous
clinical value for improving both the diagnosis and subsequent management of patients …
clinical value for improving both the diagnosis and subsequent management of patients …