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Structural Perspectives on Sigma-1 Receptor Function
2017The sigma-1 receptor is an enigmatic ER-resident transmembrane protein linked to a variety of human diseases. Although the receptor was first cloned 20 years ago, the molecular structure of the protein and the mechanistic basis for its interaction with drug-like small molecules have remained unclear until recently.
Assaf, Alon +3 more
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Sigma-1 receptor and amyotrophic lateral sclerosis
Neurology, 2018Sigma-1 receptor (Sig-1R, σ1R, also referred to as sigma receptor 1, SigR1) is an endoplasmic reticulum (ER) protein that is specifically located at the mitochondria-associated ER membrane (MAM), which interfaces between the ER and mitochondria. At the level of MAM, Sig-1R functions as a molecular chaperone that ensures proper calcium (Ca2+) transfer ...
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Structural Features Important for .sigma.1 Receptor Binding
Journal of Medicinal Chemistry, 1994Two problems that have hampered sigma receptor research are (i) a lack of high-affinity agents and (ii) the recent identification of multiple populations of sigma receptors (i.e., sigma 1 and sigma 2 sites). Recently, several high-affinity sigma ligands have been identified, and the term superpotent sigma ligands has been coined to describe agents with
R A, Glennon +5 more
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Sigma-1 Receptor and Neuronal Excitability
2017The sigma-1 receptor (Sig-1R), via interaction with various proteins, including voltage-gated and ligand-gated ion channels (VGICs and LGICs), is involved in a plethora of neuronal functions. This capability to regulate a variety of ion channel targets endows the Sig-1R with a powerful capability to fine tune neuronal excitability, and thereby the ...
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Sigma-1 Receptors Modulate NMDA Receptor Function
2013The sigma-1 receptor (σ-1R) is an endoplasmic reticulum (ER) protein that modulates a number of ion channels. It is hypothesized that σ-1Rs activated with agonist translocate to the plasma membrane. The σ-1R potentiates N-methyl-D-aspartate Receptors (NMDARs), important constituents of synaptic plasticity.
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The Sigma-1 Receptor—Orphan No More
Science Signaling, 2009An endogenous compound is a ligand for a ubiquitously expressed receptor that binds many synthetic drugs and has been implicated in psychiatric disease.
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Chapter 1. Sigma Receptors and their Ligands: The Sigma Enigma
1993Publisher Summary This chapter discusses the debate that continues over whether σ sites are true receptors or a membrane bound enzyme. Although σ receptors have been implicated in the regulation of neurotransmitter release, known neurotransmitters do not bind at σ sites. Neuropeptide Y (NPY) and peptide YY also bind at σ sites.
Magid Abou-Gharbia +2 more
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Targeting Sigma 1 receptor in Alzheimer's disease
2023The broad, long-term objective of this grant application is to understand the mechanisms involved in neuroprotective action of sigma 1 receptor (S1R) agonists Alzheimer’s disease (AD). Recent clinical and preclinical data suggest that activation of S1R may promote neuronal resilience and result in synaptoprotective and neuroprotective effects within ...
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Sigma-1 (σ1) Receptor in Memory and Neurodegenerative Diseases
2017The sigma-1 (σ1) receptor has been associated with regulation of intracellular Ca2+ homeostasis, several cellular signaling pathways, and inter-organelle communication, in part through its chaperone activity. In vivo, agonists of the σ1 receptor enhance brain plasticity, with particularly well-described impact on learning and memory. Under pathological
Maurice, Tangui, Goguadze, Nino
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