Recent advances in the development of sigma receptor ligands as cytotoxic agents: A medicinal chemistry perspective

AN Fallica, V Pittalà, MN Modica… - Journal of Medicinal …, 2021 - ACS Publications
Since their discovery as distinct receptor proteins, the specific physiopathological role of
sigma receptors (σRs) has been deeply investigated. It has been reported that these …

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 …

Targeting sigma receptors for the treatment of neurodegenerative and neurodevelopmental disorders

DS Malar, P Thitilertdecha, KS Ruckvongacheep… - CNS drugs, 2023 - Springer
The sigma-1 receptor is a 223 amino acid-long protein with a recently identified structure.
The sigma-2 receptor is a genetically unrelated protein with a similarly shaped binding …

Discovery of investigational drug CT1812, an antagonist of the sigma-2 receptor complex for Alzheimer's disease

GM Rishton, GC Look, ZJ Ni, J Zhang… - ACS Medicinal …, 2021 - ACS Publications
An unbiased phenotypic neuronal assay was developed to measure the synaptotoxic effects
of soluble Aβ oligomers. A collection of CNS druglike small molecules prepared by …

[HTML][HTML] Exosomes: Insights and therapeutic applications in cancer

AR Panigrahi, L Srinivas, J Panda - Translational Oncology, 2022 - Elsevier
Cancer refers to the division of abnormal cells at an uncontrollable rate that possesses the
ability to infiltrate and destroy normal tissues. It frequently spreads to normal tissues …

Sigma1 pharmacology in the context of cancer

FJ Kim, CM Maher - Sigma Proteins: Evolution of the Concept of Sigma …, 2017 - Springer
Sigma1 (also known as sigma-1 receptor, Sig1R, σ1 receptor) is a unique pharmacologically
regulated integral membrane chaperone or scaffolding protein. The majority of publications …

Discovery of WLB-89462, a New Drug-like and Highly Selective σ2 Receptor Ligand with Neuroprotective Properties

U Christmann, JL Díaz, R Pascual… - Journal of Medicinal …, 2023 - ACS Publications
The synthesis and pharmacological activity of a new series of isoxazolylpyrimidines as
sigma-2 receptor (σ2R) ligands are reported. Modification of a new hit retrieved in an HTS …

Proceedings from the fourth international symposium on σ-2 receptors: Role in health and disease

NJ Izzo, M Colom-Cadena, AA Riad, J Xu, M Singh… - eneuro, 2020 - eneuro.org
Abstract The σ-2 receptor (S2R) complex has been implicated in CNS disorders ranging
from anxiety and depression to neurodegenerative disorders such as Alzheimer's disease …

Cytotoxic sigma-2 ligands trigger cancer cell death via cholesterol-induced-ER-stress

R Takchi, BC Prudner, Q Gong, T Hagi… - Cell Death & …, 2024 - nature.com
Abstract Sigma-2-ligands (S2L) are characterized by high binding affinities to their cognate
sigma-2 receptor, overexpressed in rapidly proliferating tumor cells. As such, S2L were …

Quo vadis PGRMC? Grand-scale biology in human health and disease

MA Cahill - Frontiers in Bioscience-Landmark, 2022 - researchoutput.csu.edu.au
The title usage of Latin Quo vadis 'where are you going'extends the question Unde venisti
from where 'did you come?'posed in the accompanying paper and extends consideration of …