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https://www.readbyqxmd.com/read/28811536/ige-trimers-drive-spe-7-cytokinergic-activity
#1
Heather J Bax, Holly Bowen, Rebecca L Beavil, Raymond Chung, Malcolm Ward, Anna M Davies, Tihomir S Dodev, James M McDonnell, Andrew J Beavil, Brian J Sutton, Hannah J Gould
Degranulation of mast cells and basophils, with release of agents of the allergic response, ensues when multivalent antigens bind to and cross-link the cells' receptor-bound IgE antibodies. A widely used commercial monoclonal IgE antibody, SPE-7 IgE from Sigma, was found to possess the radically anomalous property, termed "cytokinergic", of inducing basophil degranulation without the intervention of an antigen. We show here that the IgE monomer, freed of protein contaminants, is devoid of this activity, and that the source of the anomaly is a trace impurity, identified as a dissociation-resistant IgE trimer...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28792792/the-effect-of-rgd-ngr-peptide-modification-of-melanoma-differentiation-associated-gene-7-interleukin-24-on-its-receptor-attachment-an-in-silico-analysis
#2
Samaneh Bina, Seyed Younes Hosseini, Fatemeh Shenavar, Ebrahim Hosseini, Mojtaba Mortazavi
Melanoma differentiation-associated gene-7 (mda-7/interleukin [IL]-24), a unique tumor suppressor gene, induces selective apoptosis in tumor cells. Secreted IL-24 binds to heterodimeric receptor complexes of IL-20R1/IL-20R2, IL-22R1/IL-20R2, or sigma-1 receptor (Sig1R) that consequently enhances apoptosis. However, this mechanism is not well understood and most likely involves different pathways. Targeting of cytokine by tumor homing peptides (THPs) to the tumor cell surface molecule-like integrin shows to be beneficial in gene immunotherapy approaches...
August 9, 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28791385/sigma-1-receptor-activation-ameliorates-anxiety-like-behavior-through-nr2a-creb-bdnf-signaling-pathway-in-a-rat-model-submitted-to-single-prolonged-stress
#3
Li-Li Ji, Jun-Bo Peng, Chang-Hai Fu, Lei Tong, Zhen-Yu Wang
Accumulating evidence has demonstrated that the σ-1 receptor (σ‑1R) possesses neuroprotective effects and is a potential novel therapeutic target for certain psychiatric diseases, including post‑traumatic stress disorder (PTSD) accompanied with anxiety disorder. It has been reported that σ‑1R agonist treatment could be modulated by the brain‑derived neurotrophic factor (BDNF) signaling pathway. However, it remains unclear whether BDNF and its upstream regulator are mechanistically involved in the therapeutic effect of σ‑1R in PTSD...
August 7, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28767411/sigma-1-and-sigma-2-receptor-ligands-induce-apoptosis-and-autophagy-but-have-opposite-effect-on-cell-proliferation-in-uveal-melanoma
#4
Lucia Longhitano, Carlo Castruccio Castracani, Daniele Tibullo, Roberto Avola, Maria Viola, Giuliano Russo, Orazio Prezzavento, Agostino Marrazzo, Emanuele Amata, Michele Reibaldi, Antonio Longo, Andrea Russo, Nunziatina Laura Parrinello, Giovanni Li Volti
Uveal melanoma is the most common primary intraocular tumor in adults, with about 1200-1500 new cases occurring per year in the United States. Metastasis is a frequent occurrence in uveal melanoma, and outcomes are poor once distant spread occurs and no clinically significant chemotherapeutic protocol is so far available. The aim of the present study was to test the effect of various σ1 and σ2 receptor ligands as a possible pharmacological strategy for this rare tumor. Human uveal melanoma cells (92.1) were treated with various concentrations of different σ2 ligands (haloperidol and haloperidol metabolite II) and σ1 ligand ((+)-pentazocine) at various concentrations (1, 10 and 25 μM) and time points (0, 4 h, 8 h, 24 h and 48 h)...
July 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28756263/synthesis-and-pharmacological-evaluation-of-benzamide-derivatives-as-potent-and-selective-sigma-1-protein-ligands
#5
Marion Donnier-Maréchal, Pascal Carato, Paul-Emmanuel Larchanché, Séverine Ravez, Rajaa Boulahjar, Amélie Barczyk, Bénédicte Oxombre, Patrick Vermersch, Patricia Melnyk
A series of novel benzamide-derived compounds was designed, synthesized and pharmacologically evaluated. Among all 37 synthesized compounds, two series were developed with the modulation of the nature, the position of atoms or groups on the benzamide scaffold, but also the nature of the amine group separated from the benzamide with 2, 3 or 4 methylene groups. In vitro competition binding assays against sigma proteins (sigma-1 S1R and sigma-2 S2R) revealed that most of them conferred S2R/S1R selectivity toward without cytotoxic effects on SY5Y cells, especially with the first series with compounds 7a-z...
July 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28756230/haloperidol-a-sigma-receptor-1-antagonist-promotes-ferroptosis-in-hepatocellular-carcinoma-cells
#6
Tao Bai, Shuai Wang, Yipu Zhao, Rongtao Zhu, Weijie Wang, Yuling Sun
Ferroptosis is a novel form of cell death, which is characterized by accumulation of reactive oxygen species (ROS). Sigma 1 receptor (S1R) has been suggested to function in oxidative stress metabolism. Both erastin and sorafenib significantly induced S1R protein expression. Haloperidol strongly promoted erastin- and sorafenib-induced cell death, which was blocked by ferrostatin-1 but not ZVAD-FMK or necrosulfonamide. During ferroptosis, haloperidol substantially increased the cellular levels of Fe(2+), GSH and lipid peroxidation...
July 26, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28752900/aberrant-astrocytic-expression-of-chondroitin-sulfate-proteoglycan-receptors-in-a-rat-model-of-amyotrophic-lateral-sclerosis
#7
Tomomi Shijo, Hitoshi Warita, Naoki Suzuki, Yasuo Kitajima, Kensuke Ikeda, Tetsuya Akiyama, Hiroya Ono, Shio Mitsuzawa, Ayumi Nishiyama, Rumiko Izumi, Masashi Aoki
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease. Progressive and systemic loss of motor neurons with gliosis in the central nervous system (CNS) is a neuropathological hallmark of ALS. Chondroitin sulfate proteoglycans (CSPGs) are the major components of the extracellular matrix of the mammalian CNS, and they inhibit axonal regeneration physically by participating to form the glial scar. Recently, protein tyrosine phosphatase sigma (PTPσ) and leukocyte common antigen-related protein were discovered as CSPG receptors that play roles in inhibiting regeneration...
July 28, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28750582/efficacy-and-safety-of-min-101-a-12-week-randomized-double-blind-placebo-controlled-trial-of-a-new-drug-in-development-for-the-treatment-of-negative-symptoms-in-schizophrenia
#8
Michael Davidson, Jay Saoud, Corinne Staner, Nadine Noel, Elisabeth Luthringer, Sandra Werner, Joseph Reilly, Jean-Yves Schaffhauser, Jonathan Rabinowitz, Mark Weiser, Remy Luthringer
OBJECTIVE: The authors assessed the efficacy, safety, and tolerability of MIN-101, a compound with affinities for sigma-2 and 5-HT2A receptors and no direct dopamine affinities, in comparison with placebo in treating negative symptoms in stabilized patients with schizophrenia. METHOD: The trial enrolled 244 patients who had been symptomatically stable for at least 3 months and had scores of at least 20 on the negative subscale of the Positive and Negative Syndrome Scale (PANSS)...
July 28, 2017: American Journal of Psychiatry
https://www.readbyqxmd.com/read/28745394/opioids-for-chronic-non-cancer-pain-in-children-and-adolescents
#9
REVIEW
Tess E Cooper, Emma Fisher, Andrew L Gray, Elliot Krane, Navil Sethna, Miranda Al van Tilburg, Boris Zernikow, Philip J Wiffen
BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past, pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as importantWe designed a suite of seven reviews on chronic non-cancer pain and cancer pain (looking at antidepressants, antiepileptic drugs, non-steroidal anti-inflammatory drugs, opioids, and paracetamol as priority areas) in order to review the evidence for children's pain utilising pharmacological interventions in children and adolescents...
July 26, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28723387/sigma-1-receptor-activation-modifies-intracellular-calcium-exchange-in-the-g93a-hsod1-als-model
#10
Vedrana Tadić, Ayse Malci, Nadine Goldhammer, Beatrice Stubendorff, Saikata Sengupta, Tino Prell, Silke Keiner, Jingyu Liu, Madlen Guenther, Christiane Frahm, Otto W Witte, Julian Grosskreutz
Aberrations in intracellular calcium (Ca(2+)) have been well established within amyotrophic lateral sclerosis (ALS), a severe motor neuron disease. Intracellular Ca(2+) concentration is controlled in part through the endoplasmic reticulum (ER) mitochondria Ca(2+) cycle (ERMCC). The ER supplies Ca(2+) to the mitochondria at close contacts between the two organelles, i.e. the mitochondria-associated ER membranes (MAMs). The Sigma 1 receptor (Sig1R) is enriched at MAMs, where it acts as an inter-organelle signaling modulator...
July 16, 2017: Neuroscience
https://www.readbyqxmd.com/read/28716934/sigma-1-receptors-control-immune-driven-peripheral-opioid-analgesia-during-inflammation-in-mice
#11
Miguel A Tejada, Angeles Montilla-García, Shane J Cronin, Domagoj Cikes, Cristina Sánchez-Fernández, Rafael González-Cano, M Carmen Ruiz-Cantero, Josef M Penninger, José M Vela, José M Baeyens, Enrique J Cobos
Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonists BD-1063 and S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute (3 h) inflammation...
August 1, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28702490/sigma-2-receptor-ligands-qsar-model-dataset
#12
Antonio Rescifina, Giuseppe Floresta, Agostino Marrazzo, Carmela Parenti, Orazio Prezzavento, Giovanni Nastasi, Maria Dichiara, Emanuele Amata
The data have been obtained from the Sigma-2 Receptor Selective Ligands Database (S2RSLDB) and refined according to the QSAR requirements. These data provide information about a set of 548 Sigma-2 (σ2) receptor ligands selective over Sigma-1 (σ1) receptor. The development of the QSAR model has been undertaken with the use of CORAL software using SMILES, molecular graphs and hybrid descriptors (SMILES and graph together). Data here reported include the regression for σ2 receptor pKi QSAR models. The QSAR model was also employed to predict the σ2 receptor pKi values of the FDA approved drugs that are herewith included...
August 2017: Data in Brief
https://www.readbyqxmd.com/read/28700244/targeted-yttrium-89-doxorubicin-drug-eluting-bead-a-safety-and-feasibility-pilot-study-in-a-rabbit-liver-cancer-model
#13
Johannes M Ludwig, Minzhi Xing, Yongkang Gai, Lingyi Sun, Dexing Zeng, Hyun S Kim
The purpose of this article is to evaluate feasibility and safety of the cancer targeting (radio)-chemoembolization drug-eluting bead (TRCE-DEB) concept drug SW43-DOX-L-NETA((89)Y) DEB for the intra-arterial treatment of VX2 rabbit liver tumors. The treatment compound comprises of the sigma-2 receptor ligand SW43 for cancer targeting, doxorubicin (DOX), and (89)yttrium ((89)Y) as nonradioactive surrogate for therapeutic (yttrium-90, lutetium-177) and imaging (yttrium-86) radioisotopes via the chelator L-NETA...
August 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28687423/an-increase-of-sigma-1-receptor-in-the-penumbra-neuron-after-acute-ischemic-stroke
#14
Xiaotian Zhang, Fangfang Wu, Yun Jiao, Tianyu Tang, Li Yang, Chunqiang Lu, Yanhong Zhang, Yuan Zhang, Ying Bai, Jie Chao, Gaojun Teng, Honghong Yao
BACKGROUND: Penumbra salvage from infarction by early reperfusion within the time window is the target of acute ischemic stroke therapies. Although the penumbral imaging is potently usable in clinic trial, additional work needs to be performed to advancing the field with better-defined, evaluated, and validated imaging measures. METHODS: Mice were subjected to permanent stroke by right middle cerebral artery (MCA) occlusion. Multimodel magnetic resonance imaging (MRI) method was assessed to define the penumbra as that brain region in which the perfusion and diffusion-weighted MR images are mismatched (perfusion-weighted imaging [PWI]-diffusion-weighted imaging [DWI] mismatch)...
September 2017: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/28682953/role-of-sigma-1-receptor-p38-mapk-inhibition-in-acupoint-catgut-embedding-mediated-analgesic-effects-in-complete-freund-s-adjuvant-induced-inflammatory-pain
#15
Kairong Du, Xue Wang, Laiting Chi, Wenzhi Li
BACKGROUND: The endoplasmic reticulum chaperone protein Sigma-1 receptor (Sig-1 R) and mitogen-activated protein kinases (MAPKs) are involved in the mechanism of pain. Acupoint stimulation exerts an exact antihyperalgesic effect in inflammatory pain. However, whether Sig-1 R and MAPKs are associated with the acupoint stimulation-induced analgesic effects is not clear. This study investigated the analgesic effect of acupoint catgut embedding (ACE) and the inhibition of Sig-1 R and MAPKs in ACE analgesia...
August 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28667101/sigmar1-regulates-endoplasmic-reticulum-stress-induced-c-ebp-homologous-protein-chop-expression-in-cardiomyocytes
#16
Shafiul Alam, Chowdhury S Abdullah, Richa Aishwarya, A Wayne Orr, James Traylor, Sumitra Miriyala, Manikandan Panchatcharam, Christopher B Pattillo, Md Shenuarin Bhuiyan
C/EBP-homologous protein (CHOP) is a ubiquitously expressed stress-inducible transcription factor robustly induced by maladaptive endoplasmic reticulum (ER) stresses in a wide variety of cells. Here we examined a novel function of Sigma 1 receptor (Sigmar1) in regulating CHOP expression under ER-stress in cardiomyocytes. We also defined Sigmar1-dependent activation of the adaptive ER-stress pathway in regulating CHOP expression. We used adenovirus-mediated Sigmar1 overexpression as well as Sigmar1 knockdown by small interfering RNA (siRNA) in neonatal rat ventricular cardiomyocytes; to induce ER-stress cardiomyocytes were treated with tunicamycin...
June 30, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28654186/haloperidol-decreases-hyperalgesia-and-allodynia-induced-by-chronic-constriction-injury
#17
Josué Vidal Espinosa-Juárez, Osmar Antonio Jaramillo-Morales, Francisco Javier López-Muñoz
Neuropathic pain has proven to be a difficult condition to treat, so investigational therapy has been sought that may prove useful, such as the use of sigma-1 antagonists. Haloperidol (HAL) is a compound that shows a high affinity with these receptors, acting as an antagonist. Therefore, the objective of this study was to demonstrate its effect in an experimental model of neuropathic pain and corroborate its antagonistic action of the sigma-1 receptors under these conditions. BD-1063 was used as a sigma-1 antagonist control and gabapentin was used as a positive control...
June 27, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28648406/n-2-morpholin-4-yl-ethyl-2-1naphthyloxy-acetamide-inhibits-the-chronic-constriction-injury-generated-hyperalgesia-via-the-antagonism-of-sigma-1-receptors
#18
Josué Vidal Espinosa-Juárez, Osmar Antonio Jaramillo-Morales, Gabriel Navarrete-Vázquez, Luis Alberto Melo Hernández, Myrna Déciga-Campos, Francisco Javier López-Muñoz
The most used therapeutic treatment to relieve neuropathic pain is that of neuromodulators such as anti-epileptics or anti-depressants; however, there are alternatives that may be potentially useful. The sigma-1 receptor is a therapeutic target that has shown favorable results at preclinical levels. The aim of this study was to evaluate the anti-hyperalgesic effect of N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy) acetamide (NMIN) in a chronic constriction injury model (CCI) and compare it both a sigma-1 antagonist (BD-1063) and also Gabapentin, as well as determine its possible role as an antagonist of sigma-1 receptors...
June 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28644012/sigma-2-receptor-tmem97-agonists-produce-long-lasting-antineuropathic-pain-effects-in-mice
#19
James J Sahn, Galo L Mejia, Pradipta R Ray, Stephen F Martin, Theodore J Price
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and antagonists for this receptor are effective in preclinical models and are currently in phase II clinical trials. Conversely, relatively little is known about σ2R, which has recently been identified as transmembrane protein 97 (Tmem97). We generated a series of σ1R and σ2R/Tmem97 agonists and antagonists and tested them for efficacy in the mouse spared nerve injury (SNI) model...
August 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28622300/the-als-linked-e102q-mutation-in-sigma-receptor-1-leads-to-er-stress-mediated-defects-in-protein-homeostasis-and-dysregulation-of-rna-binding-proteins
#20
Alice Dreser, Jan Tilmann Vollrath, Antonio Sechi, Sonja Johann, Andreas Roos, Alfred Yamoah, Istvan Katona, Saeed Bohlega, Dominik Wiemuth, Yuemin Tian, Axel Schmidt, Jörg Vervoorts, Marc Dohmen, Cordian Beyer, Jasper Anink, Eleonora Aronica, Dirk Troost, Joachim Weis, Anand Goswami
Amyotrophic lateral sclerosis (ALS) is characterized by the selective degeneration of motor neurons (MNs) and their target muscles. Misfolded proteins which often form intracellular aggregates are a pathological hallmark of ALS. Disruption of the functional interplay between protein degradation (ubiquitin proteasome system and autophagy) and RNA-binding protein homeostasis has recently been suggested as an integrated model that merges several ALS-associated proteins into a common pathophysiological pathway...
June 16, 2017: Cell Death and Differentiation
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