Sigma-1 (σ1) Receptor in Memory and Neurodegenerative Diseases

2017 ◽  
pp. 81-108 ◽  
Author(s):  
Tangui Maurice ◽  
Nino Goguadze
Keyword(s):  
Neurodegenerative Diseases ◽  
Σ1 Receptor ◽  
Sigma 1

scholarly journals 3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (σ1) receptor

2013 ◽  
Vol 23 (6) ◽  
pp. 1707-1711 ◽  
Author(s):  
Werner J. Geldenhuys ◽  
Nicholas Novotny ◽  
Sarel F. Malan ◽  
Cornelis J. Van der Schyf
Keyword(s):  
3D Qsar ◽  
Docking Studies ◽  
Σ1 Receptor ◽  
Sigma 1

scholarly journals Sigma-1 (σ1) receptor activity is necessary for physiological brain plasticity in mice

2020 ◽  
Vol 39 ◽  
pp. 29-45 ◽  
Author(s):  
Lucie Crouzier ◽  
Simon Couly ◽  
Chloé Roques ◽  
Coralie Peter ◽  
Rislen Belkhiter ◽  
...  
Keyword(s):  
Brain Plasticity ◽  
Receptor Activity ◽  
Σ1 Receptor ◽  
Sigma 1

scholarly journals Role of sigma-1 receptors in neurodegenerative diseases

2015 ◽  
Vol 127 (1) ◽  
pp. 17-29 ◽  
Author(s):  
Linda Nguyen ◽  
Brandon P. Lucke-Wold ◽  
Shona A. Mookerjee ◽  
John Z. Cavendish ◽  
Matthew J. Robson ◽  
...  
Keyword(s):  
Neurodegenerative Diseases ◽  
Sigma 1

scholarly journals Multi-Target Directed Ligands (MTDLs) Binding the σ1 Receptor as Promising Therapeutics: State of the Art and Perspectives

2021 ◽  
Vol 22 (12) ◽  
pp. 6359
Author(s):  
Francesca Serena Abatematteo ◽  
Mauro Niso ◽  
Marialessandra Contino ◽  
Marcello Leopoldo ◽  
Carmen Abate
Keyword(s):  
Winning Strategy ◽  
Endoplasmic Reticulum Membrane ◽  
Proof Of Concept ◽  
Σ1 Receptor ◽  
Chaperone Protein ◽  
Sigma 1 ◽  
Membrane Interfaces ◽  
Client Proteins ◽  
Physiological Pathways ◽  
Multifunctional Ligands

The sigma-1 (σ1) receptor is a ‘pluripotent chaperone’ protein mainly expressed at the mitochondria–endoplasmic reticulum membrane interfaces where it interacts with several client proteins. This feature renders the σ1 receptor an ideal target for the development of multifunctional ligands, whose benefits are now recognized because several pathologies are multifactorial. Indeed, the current therapeutic regimens are based on the administration of different classes of drugs in order to counteract the diverse unbalanced physiological pathways associated with the pathology. Thus, the multi-targeted directed ligand (MTDL) approach, with one molecule that exerts poly-pharmacological actions, may be a winning strategy that overcomes the pharmacokinetic issues linked to the administration of diverse drugs. This review aims to point out the progress in the development of MTDLs directed toward σ1 receptors for the treatment of central nervous system (CNS) and cancer diseases, with a focus on the perspectives that are proper for this strategy. The evidence that some drugs in clinical use unintentionally bind the σ1 protein (as off-target) provides a proof of concept of the potential of this strategy, and it strongly supports the promise that the σ1 receptor holds as a target to be hit in the context of MTDLs for the therapy of multifactorial pathologies.

Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ1) receptor ligands with potent anti-amnesic effect

2021 ◽  
pp. 114038
Author(s):  
Francesca S. Abatematteo ◽  
Philip D. Mosier ◽  
Mauro Niso ◽  
Leonardo Brunetti ◽  
Francesco Berardi ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Amnesic Effect ◽  
High Affinity ◽  
Σ1 Receptor ◽  
Sigma 1

High-affinity sigma-1 (σ1) receptor ligands based on the σ1 antagonist PB212

2019 ◽  
Vol 11 (19) ◽  
pp. 2547-2562 ◽  
Author(s):  
Mauro Niso ◽  
Philip D Mosier ◽  
Roberta Marottoli ◽  
Savina Ferorelli ◽  
Giuseppe Cassano ◽  
...  
Keyword(s):  
Pharmacophore Model ◽  
Therapeutic Benefit ◽  
Calcium Flux ◽  
Structural Basis ◽  
Therapeutic Drug ◽  
Receptor Ligands ◽  
Σ1 Receptor ◽  
Physiological Processes ◽  
Sigma 1 ◽  
New Compounds

Aim: The σ1 receptor is a druggable target involved in many physiological processes and diseases. To clarify its physiology and derive therapeutic benefit, nine analogs based on the σ1 antagonist PB212 were synthesized replacing the 4-methylpiperidine with basic moieties of varying size and degree of conformational freedom. Results & methodology: 3-Phenylpyrrolidine, 4-phenylpiperidine or granatane derivatives displayed the highest affinity ( Ki.#x00A0;= 0.12, 0.31 or 1.03 nM). Calcium flux assays in MCF7σ1 cells indicated that the highest σ1 receptor affinity are σ1 antagonists. Molecular models provided a structural basis for understanding the σ1 affinity and functional activity of the analogs and incorporated Glennon's σ1 pharmacophore model. Conclusion: Herein, we identify new compounds exploitable as therapeutic drug leads or as tools to study σ1 receptor physiology.

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