Sigma-2 receptors—From basic biology to therapeutic target: A focus on age-related degenerative diseases

BN Lizama, J Kahle, SM Catalano… - International journal of …, 2023 - mdpi.com
There is a large unmet medical need to develop disease-modifying treatment options for
individuals with age-related degenerative diseases of the central nervous system. The …

The sigma receptors in Alzheimer's disease: New potential targets for diagnosis and therapy

T Wang, H Jia - International Journal of Molecular Sciences, 2023 - mdpi.com
Sigma (σ) receptors are a class of unique proteins with two subtypes: the sigma-1 (σ1)
receptor which is situated at the mitochondria-associated endoplasmic reticulum (ER) …

Computational chemistry for the identification of lead compounds for radiotracer development

CJ Hsieh, S Giannakoulias, EJ Petersson, RH Mach - Pharmaceuticals, 2023 - mdpi.com
The use of computer-aided drug design (CADD) for the identification of lead compounds in
radiotracer development is steadily increasing. Traditional CADD methods, such as structure …

A Novel Brain PET Radiotracer for Imaging Alpha Synuclein Fibrils in Multiple System Atrophy

HY Kim, WK Chia, CJ Hsieh… - Journal of Medicinal …, 2023 - ACS Publications
Abnormal α-synuclein (α-syn) aggregation characterizes α-synucleinopathies, including
Parkinson's disease (PD) and multiple system atrophy (MSA). However, no suitable positron …

Characterization of CM-398, a novel selective sigma-2 receptor ligand, as a potential therapeutic for neuropathic pain

LL Wilson, AR Alleyne, SO Eans, TJ Cirino, HM Stacy… - Molecules, 2022 - mdpi.com
Sigma receptors modulate nociception, offering a potential therapeutic target to treat pain,
but relatively little is known regarding the role of sigma-2 receptors (S2R) in nociception. The …

Exploration of Diazaspiro Cores as Piperazine Bioisosteres in the Development of σ2 Receptor Ligands

K Xu, CJ Hsieh, JY Lee, A Riad, NJ Izzo… - International Journal of …, 2022 - mdpi.com
A series of σ2R compounds containing benzimidazolone and diazacycloalkane cores was
synthesized and evaluated in radioligand binding assays. Replacing the piperazine moiety …

Development and Optimization of 11C-Labeled Radiotracers: A Review of the Modern Quality Control Design Process

PJ Myburgh, KKS Sai - ACS Pharmacology & Translational …, 2023 - ACS Publications
Introduction-Several 11C-tracers have demonstrated high potential in early diagnostic PET
imaging applications of neurodegenerative diseases including Alzheimer's and Parkinson's …

Diagnostic and therapeutic radiopharmaceuticals

CW Lindsley, CE Müller… - ACS Pharmacology & …, 2022 - ACS Publications
Radiopharmaceuticals labeled with positron emission tomography (PET) and single-photon
emission computed tomography (SPECT) radionuclides have demonstrated high efficiency …

Identification of novel tau positron emission tomography tracers for chronic traumatic encephalopathy by comprehensive in silico screening and molecular dynamics …

B Qi, L Guan, J Tan, G Li, Y Sun, Q Zhang… - Physical Chemistry …, 2025 - pubs.rsc.org
Chronic traumatic encephalopathy (CTE), a neurodegenerative disease associated with
repetitive mild traumatic brain injury, is characterized neuropathologically by abnormal …

Evaluation of a First PET Tracer Suitable for Imaging the Sigma-2 Receptor in the Brain of Nonhuman Primates

SR Alluri, MQ Zheng, D Holden, Y Zhang… - Molecular …, 2023 - ACS Publications
The sigma-2 receptor (σ2R), recently identified as transmembrane protein 97, is expressed
in many cell types and mediates important functions in both the peripheral and central …