PET molecular imaging in drug development: the imaging and chemistry perspective

SG Nerella, P Singh, T Sanam, CS Digwal - Frontiers in Medicine, 2022 - frontiersin.org
Positron emission tomography with selective radioligands advances the drug discovery and
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) …

Physiological blood–brain transport is impaired with age by a shift in transcytosis

AC Yang, MY Stevens, MB Chen, DP Lee, D Stähli… - Nature, 2020 - nature.com
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 …

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 …

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 …

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 …

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 …

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 …

[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 …

[HTML][HTML] Visualizing nerve injury in a neuropathic pain model with [18F] FTC-146 PET/MRI

B Shen, D Behera, ML James, ST Reyes, L Andrews… - Theranostics, 2017 - ncbi.nlm.nih.gov
The ability to locate nerve injury and ensuing neuroinflammation would have tremendous
clinical value for improving both the diagnosis and subsequent management of patients …