scholarly journals A systematic exploration of the effects of flexibility and basicity on sigma (σ) receptor binding in a series of substituted diamines

2016 ◽  
Vol 14 (39) ◽  
pp. 9388-9405 ◽  
Author(s):  
Trent Conroy ◽  
Madhura Manohar ◽  
Yu Gong ◽  
Shane M. Wilkinson ◽  
Michael Webster ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Neurological Disorders ◽  
Open Chain ◽  
Sigma 1 Receptor ◽  
Systematic Exploration ◽  
Sigma 1

Investigating amide and open chain piperazine analogues to target the sigma 1 receptor to fight neurological disorders.

scholarly journals Syntheses of 7-Substituted α-Cyperone Derivatives for Selective Sigma-1 Receptor over Cannabinoid-1 Receptor Binding Affinities

2013 ◽  
Vol 34 (11) ◽  
pp. 3499-3502
Author(s):  
Ju-Young Park ◽  
Young-Gyun Shin ◽  
Kee-Won Kim ◽  
Young-Bae Kwon ◽  
Sung-Hwa Yoon
Keyword(s):  
Receptor Binding ◽  
Binding Affinities ◽  
Sigma 1 Receptor ◽  
Cannabinoid 1 Receptor ◽  
Sigma 1

Novel Radioligands for Sigma‐1 Receptor Binding Studies

2008 ◽  
Vol 22 (S2) ◽  
pp. 628-628
Author(s):  
james A Fishback ◽  
Christophe Mesangeau ◽  
Sanju Narayanan ◽  
Christopher R McCurdy ◽  
Rae R Matsumoto
Keyword(s):  
Receptor Binding ◽  
Binding Studies ◽  
Sigma 1 Receptor ◽  
Sigma 1

scholarly journals Sigma-1 Receptor: A Potential Therapeutic Target for Traumatic Brain Injury

2021 ◽  
Vol 15 ◽  
Author(s):  
Mingming Shi ◽  
Fanglian Chen ◽  
Zhijuan Chen ◽  
Weidong Yang ◽  
Shuyuan Yue ◽  
...  
Keyword(s):  
Traumatic Brain Injury ◽  
Endoplasmic Reticulum ◽  
Brain Injury ◽  
Neurological Disorders ◽  
Inflammatory Responses ◽  
Current Knowledge ◽  
Glutamate Excitotoxicity ◽  
Sigma 1 Receptor ◽  
Beneficial Effects ◽  
Sigma 1

The sigma-1 receptor (Sig-1R) is a chaperone receptor that primarily resides at the mitochondria-associated endoplasmic reticulum (ER) membrane (MAM) and acts as a dynamic pluripotent modulator regulating cellular pathophysiological processes. Multiple pharmacological studies have confirmed the beneficial effects of Sig-1R activation on cellular calcium homeostasis, excitotoxicity modulation, reactive oxygen species (ROS) clearance, and the structural and functional stability of the ER, mitochondria, and MAM. The Sig-1R is expressed broadly in cells of the central nervous system (CNS) and has been reported to be involved in various neurological disorders. Traumatic brain injury (TBI)-induced secondary injury involves complex and interrelated pathophysiological processes such as cellular apoptosis, glutamate excitotoxicity, inflammatory responses, endoplasmic reticulum stress, oxidative stress, and mitochondrial dysfunction. Thus, given the pluripotent modulation of the Sig-1R in diverse neurological disorders, we hypothesized that the Sig-1R may affect a series of pathophysiology after TBI. This review summarizes the current knowledge of the Sig-1R, its mechanistic role in various pathophysiological processes of multiple CNS diseases, and its potential therapeutic role in TBI.

Structural Features Important for .sigma.1 Receptor Binding

1994 ◽  
Vol 37 (8) ◽  
pp. 1214-1219 ◽  
Author(s):  
Richard A. Glennon ◽  
Seth Y. Ablordeppey ◽  
Abd M. Ismaiel ◽  
Mahmoud B. El-Ashmawy ◽  
James B. Fischer ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Structural Features ◽  
Sigma 1 Receptor ◽  
Sigma 1

scholarly journals The effects of terminal tagging on homomeric interactions of the sigma 1 receptor

2019 ◽  
Author(s):  
Hideaki Yano ◽  
Leanne Liu ◽  
Sett Naing ◽  
Lei Shi
Keyword(s):  
Ligand Binding ◽  
Neurological Disorders ◽  
Transmembrane Segment ◽  
Cellular Functions ◽  
Migration Patterns ◽  
Terminal Ligand ◽  
Sigma 1 Receptor ◽  
C Terminus ◽  
Sigma 1 ◽  
Drug Treatments

AbstractThe sigma 1 receptor (σ1R) has been implicated in cancers, neurological disorders, and substance use disorders. Yet, its molecular and cellular functions have not been well-understood. Recent crystal structures of σ1R reveal a single N-terminal transmembrane segment and C-terminal ligand-binding domain, and a trimeric organization. Nevertheless, outstanding issues surrounding the functional or pharmacological relevance of σ1R oligomerization remain, such as the minimal protomeric unit and the differentially altered oligomerization states by different classes of ligands. Western blot (WB) assays have been widely used to investigate protein oligomerizations. However, the unique topology of σ1R renders several intertwined challenges in WB. Here we describe a WB protocol without temperature denaturization to study the ligand binding effects on the oligomerization state of σ1R. Using this approach, we observed unexpected ladder-like incremental migration pattern of σ1R, demonstrating preserved homomeric interactions in the detergent environment. We compared the migration patterns of intact σ1R construct and the C-terminally tagged σ1R constructs, and found similar trends in response to drug treatments. In contrast, N-terminally tagged σ1R constructs show opposite trends to that of the intact construct, suggesting distorted elicitation of the ligand binding effects on oligomerization. Together, our findings indicate that the N-terminus plays an important role in eliciting the impacts of bound ligands, whereas the C-terminus is amenable for modifications for biochemical studies.

scholarly journals Probing the Steroid Binding Domain-like I (SBDLI) of the Sigma-1 Receptor Binding Site Using N-Substituted Photoaffinity Labels†

Biochemistry ◽  
2008 ◽  
Vol 47 (27) ◽  
pp. 7205-7217 ◽  
Author(s):  
Dominique Fontanilla ◽  
Abdol R. Hajipour ◽  
Arindam Pal ◽  
Uyen B. Chu ◽  
Marty Arbabian ◽  
...  
Keyword(s):  
Binding Site ◽  
Receptor Binding ◽  
Binding Domain ◽  
Receptor Binding Site ◽  
Sigma 1 Receptor ◽  
Sigma 1 ◽  
Steroid Binding ◽  
Photoaffinity Labels
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