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https://www.readbyqxmd.com/read/28443084/gene-expression-profiling-of-transcription-factors-of-helicobacter-pylori-under-different-environmental-conditions
#1
Miguel A De la Cruz, Miguel A Ares, Kristine von Bargen, Leonardo G Panunzi, Jessica Martínez-Cruz, Hilda A Valdez-Salazar, César Jiménez-Galicia, Javier Torres
Helicobacter pylori is a Gram-negative bacterium that colonizes the human gastric mucosa and causes peptic ulcers and gastric carcinoma. H. pylori strain 26695 has a small genome (1.67 Mb), which codes for few known transcriptional regulators that control bacterial metabolism and virulence. We analyzed by qRT-PCR the expression of 16 transcriptional regulators in H. pylori 26695, including the three sigma factors under different environmental conditions. When bacteria were exposed to acidic pH, urea, nickel, or iron, the sigma factors were differentially expressed with a particularly strong induction of fliA...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28442581/sigma-receptor-effects-of-n-substituted-benztropine-analogs-implications-for-antagonism-of-cocaine-self-administration
#2
Takato Hiranita, Weimin C Hong, Theresa Kopajtic, Jonathan L Katz
Several N-substituted benztropine (BZT) analogs are atypical dopamine transport inhibitors as they have affinity for the dopamine transporter (DAT), but have minimal cocaine-like pharmacological effects and can block numerous effects of cocaine including its self-administration. Among these compounds, N-methyl (AHN1-055), N-allyl (AHN2-005), and N-butyl (JHW007) analogs of 3α-[bis(4'-fluorophenyl)methoxy]-tropane were more potent in antagonizing self-administration of cocaine and d-methamphetamine than in decreasing food-maintained responding...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28440951/concluding-the-trilogy-the-interaction-of-2-2-dihydroxy-benzophenones-and-their-carbonyl-n-analogues-with-human-glutathione-transferase-m1-1-face-to-face-with-the-p1-1-and-a1-1-isoenzymes-involved-in-mdr
#3
Nikolaos D Georgakis, Dionisis A Karagiannopoulos, Trias N Thireou, Elias E Eliopoulos, Nikolaos E Labrou, Petros G Tsoungas, Michael N Koutsilieris, Yannis D Clonis
The conjugation of intracellular glutathione (GSH) with several electrophilic, predominantly hydrophobic, endogenous and xenobiotic compounds, such as chemotherapeutics and carcinogenics, agrochemicals and other drugs, is catalyzed by the multigene enzyme family of glutathione transferases (GSTs). The mammalian family of GSTs comprises three groups: cytosolic, mitochondrial and microsomal. Human cytosolic GSTs constitute the largest family, which is classified in seven distinct classes named Alpha (Α), Mu (M), Pi (P), Theta (T), Sigma (S), Zeta (Z) and Omega (O)...
April 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28435536/norbenzomorphan-scaffold-chemical-tool-for-modulating-sigma-receptor-subtype-selectivity
#4
James J Sahn, Timothy R Hodges, Jessica Z Chan, Stephen F Martin
Some norbenzomorphans exhibit high affinity for sigma 1 and sigma 2 receptors, and varying the position of substituents on the aromatic ring of this scaffold has a significant effect on subtype selectivity. In particular, compounds bearing several different substituents at C7 of the norbenzomorphan ring system exhibit a general preference for the sigma 1 receptor, whereas the corresponding C8-substituted analogues preferentially bind at the sigma 2 receptor. These findings suggest that the norbenzomorphan scaffold may be a unique chemical template that can be easily tuned to prepare small molecules for use as tool compounds to study the specific biological effects arising from preferential binding at either sigma receptor subtype...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28432957/nanoencapsulation-strategies-for-the-delivery-of-novel-bifunctional-antioxidant-%C3%AF-1-selective-ligands
#5
Claudia Carbone, Emanuela Arena, Veronica Pepe, Orazio Prezzavento, Ivana Cacciatore, Hasan Turkez, Agostino Marrazzo, Antonio Di Stefano, Giovanni Puglisi
Nowadays sigma-1 receptors are considered as new therapeutic objectives for central nervous system neurodegenerative diseases. Among different molecules, alpha lipoic acid has been identified as a natural potent antioxidant drug, whose therapeutic efficacy is limited by its many drawbacks, such as fast metabolism, poor bioavailability and high physico-chemical instability. Alfa-lipoic acid derivatives have been recently developed demonstrating their neuroprotective activity and effectiveness in different types of oxidative stress...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28431607/sigma-1-receptor-in-brain-ischemia-reperfusion-possible-role-in-the-nr2a-induced-pathway-to-regulate-brain-derived-neurotrophic-factor
#6
Qian Xu, Xue-Fei Ji, Tian-Yan Chi, Peng Liu, Ge Jin, Ling Chen, Li-Bo Zou
Sigma-1 receptor (σ1r) activation could attenuate the learning and memory deficits in the AD model, ischemia model and others. In our previous study, the activation of σ1r increased the expression of brain-derived neurotrophic factor (BDNF), possibly through the NR2A-induced pathway, and σ1r agonists might function as neuroprotectant agents in vascular dementia. Here, we used σ1r knockout mice to confirm the role of σ1r. Furthermore, an antagonist of NR2A was first used to investigate whether the NR2A-induced pathway is the necessary link between σ1r and BDNF...
May 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28430083/hydrocephalus-treatment-in-children-long-term-outcome-in-975-consecutive-patients
#7
Pierre-Aurelien Beuriat, Stephanie Puget, Giuseppe Cinalli, Thomas Blauwblomme, Kevin Beccaria, Michel Zerah, Christian Sainte-Rose
OBJECTIVE Hydrocephalus remains one of the more common pathologies managed in pediatric neurosurgical units. Endoscopic third ventriculostomy (ETV) has an advantage over ventriculoperitoneal shunting as it enables patients to remain device free. Multiple shunt devices with various valve designs exist, with no one valve proven to be superior to another. The aim of this study was to describe the management of hydrocephalus and its long-term outcome. METHODS The authors retrospectively reviewed the medical records of all patients who had been treated for hydrocephalus at the Hôpital Necker-Enfants Malades in the period from 1985 to 1995...
April 21, 2017: Journal of Neurosurgery. Pediatrics
https://www.readbyqxmd.com/read/28421439/sigma-1-receptor-antagonist-haloperidol-attenuates-ca-2-responses-induced-by-glutoxim-and-molixan-in-macrophages
#8
Z I Krutetskaya, L S Milenina, A A Naumova, S N Butov, V G Antonov, A D Nozdrachev
Using Fura-2AM microfluorimetry, we have shown for the first time that sigma-1 receptor antagonist, antipsychotic haloperidol, significantly inhibits glutoxim- and molixan-induced Ca(2+)-response in peritoneal macrophages. These results indicate possible involvement of sigma-1 receptors in the signal cascade induced by glutoxim or molixan and leading to intracellular Ca(2+) concentration increase in macrophages.
January 2017: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28417127/on-the-formation-of-stripe-sigma-and-honeycomb-phases-in-a-core-corona-system
#9
Harini Pattabhiraman, Marjolein Dijkstra
Using Monte Carlo simulations and free-energy calculations, we investigate the phase behaviour of a two-dimensional core-corona system. We model this system as particles consisting of an impenetrable hard core of diameter σHD surrounded by a purely repulsive soft corona of diameter δ = 1.95σHD. At low densities, we observe the spontaneous formation of a phase with a stripe texture as well as a honeycomb-like phase driven by both energy and entropy considerations. At high densities, we find that a two-dimensional analogue of the periodic sigma phase, considered as an approximant of dodecagonal quasicrystals, is energetically stabilised with respect to two distinct dodecagonal quasicrystals, namely, a square-triangle tiling and a square-triangle-shield tiling...
April 18, 2017: Soft Matter
https://www.readbyqxmd.com/read/28412515/genome-wide-determination-of-transcription-start-sites-reveals-new-insights-into-promoter-structures-in-the-actinomycete-corynebacterium-glutamicum
#10
Andreas Albersmeier, Katharina Pfeifer-Sancar, Christian Rückert, Jörn Kalinowski
The genome-wide identification of transcription start sites, enabled by high-throughput sequencing of a cDNA library enriched for native 5' transcript ends, is ideally suited for the analysis of promoters. Here, the transcriptome of Corynebacterium glutamicum, a non-pathogenic soil bacterium from the actinomycetes branch that is used in industry for the production of amino acids, was analysed by transcriptome sequencing of the 5'-ends of native transcripts. Total RNA samples were harvested from the exponential phase of growth, therefore the study mainly addressed promoters recognized by the main house-keeping sigma factor σ(A)...
April 12, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28409931/1-4-18-f-fluorobenzyl-4-tetrahydrofuran-2-yl-methyl-piperazine-a-novel-suitable-radioligand-with-low-lipophilicity-for-imaging-sigma-1-receptors-in-the-brain
#11
Yingfang He, Fang Xie, Jiajun Ye, Winnie Deuther-Conrad, Bixiao Cui, Liang Wang, Jie Lu, Jörg Steinbach, Peter Brust, Yiyun Huang, Jie Lu, Hongmei Jia
We have designed and synthesized novel piperazine compounds with low lipophilicity as σ1 receptor ligands. 1-(4-Fluorobenzyl)-4-((tetrahydrofuran-2-yl)methyl)piperazine (10) possessed low nanomolar σ1 receptor affinity and high selectivity toward the vesicular acetylcholine transporter (>2000-fold), σ2 receptors (52-fold), adenosine A2A, adrenergic α2, cannabinoid CB1, dopamine D1, D2L, γ-aminobutyric acid A (GABAA), NMDA, melatonin MT1, MT2 and serotonin 5-HT1 receptors. The corresponding radiotracer [(18)F]10 demonstrated high brain uptake and extremely high brain-to-blood ratios in biodistribution studies in mice...
April 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28408317/involvement-of-puma-in-pericyte-migration-induced-by-methamphetamine
#12
Yanhong Zhang, Yuan Zhang, Ying Bai, Jie Chao, Gang Hu, Xufeng Chen, Honghong Yao
Mounting evidence indicates that methamphetamine causes blood-brain barrier damage, with emphasis on endothelial cells. The role of pericytes in methamphetamine-induced BBB damage remains unknown. Our study demonstrated that methamphetamine increased the migration of pericytes from the endothelial basement membrane. However, the detailed mechanisms underlying this process remain poorly understood. Thus, we examined the molecular mechanisms involved in methamphetamine-induced pericyte migration. The results showed that exposure of C3H/10T1/2 cells and HBVPs to methamphetamine increased PUMA expression via activation of the sigma-1 receptor, MAPK and Akt/PI3K pathways...
April 10, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28399188/the-gas6-gene-rs8191974-and-ap3s2-gene-rs2028299-are-associated-with-type-2-diabetes-in-the-northern-chinese-han-population
#13
Elena V Kazakova, Tianwei Zghuang, Tingting Li, Qingxiao Fang, Jun Han, Hong Qiao
Previous studies in other countries have shown that single nucleotide polymorphisms (SNPs) in the growth arrest-specific gene 6 (Gas6; rs8191974) and adapter-related protein complex 3 subunit sigma-2 (Ap3s2; rs2028299) were associated with an increasedrisk for type 2 diabetes mellitus (T2DM). However, the association of these loci with T2DM has not been examined in Chinese populations. We performed a replication study to investigate the association of these susceptibility loci with T2DM in the Chinese population...
April 11, 2017: Acta Biochimica Polonica
https://www.readbyqxmd.com/read/28396637/membrane-associated-progesterone-receptors-promiscuous-proteins-with-pleiotropic-functions-focus-on-interactions-with-cytochromes-p450
#14
REVIEW
Chang S Ryu, Kathrin Klein, Ulrich M Zanger
Membrane-associated progesterone receptors (MAPR) are a group of four rather small, partially homologous proteins, which share a similar non-covalent heme-binding domain that is related to cytochrome b5, a well-known functional interaction partner of microsomal cytochrome P450 (CYP) monooxygenase systems. Apart from their structural similarities the four proteins progesterone membrane component 1 (PGRMC1, also referred to as IZA, sigma-2 receptor, Dap1), PGRMC2, neudesin (NENF) and neuferricin (CYB5D2) display surprisingly divergent and multifunctional physiological properties related to cholesterol/steroid biosynthesis, drug metabolism and response, iron homeostasis, heme trafficking, energy metabolism, autophagy, apoptosis, cell cycle regulation, cell migration, neural functions, and tumorigenesis and cancer progression...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28396142/atypical-binding-at-dopamine-and-serotonin-transporters-contribute-to-the-discriminative-stimulus-effects-of-mephedrone
#15
Alyssa F DeLarge, Laura L Erwin, Peter J Winsauer
Mephedrone (4-methylmethcathinone), a constituent of the recreational substances known as "bath salts", is a synthetic cathinone that can produce auditory and visual hallucinations, as well as problematic cardiovascular effects. This study compared the discriminative stimulus effects of mephedrone (0.32-10 mg/kg) with other prototypical drugs of abuse: cocaine (0.56-32 mg/kg), d-amphetamine (0.18-3.2 mg/kg), ketamine (1.8-18 mg/kg), phencyclidine (PCP, 1-5.6 mg/kg), heroin (1-10 mg/kg), 2,5-dimethoxy-4-iodoamphetamine (R-DOI, 0...
April 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28389944/coupling-of-flagellar-gene-expression-with-assembly-in-salmonella-enterica
#16
Fabienne F V Chevance, Kelly T Hughes
There are more than 70 genes in the flagellar and chemosensory regulon of Salmonella enterica. These genes are organized into a transcriptional hierarchy of three promoter classes. At the top of the transcriptional hierarchy is the flhDC operon, also called the flagellar master operon, which is transcribed from the flagellar class 1 promoter region. The protein products of the flhDC operon form a hetero-multimeric complex, FlhD4C2, which directs σ(70) RNA polymerase to transcribe from class 2 flagellar promoters...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28389336/the-activity-of-selective-sigma-1-receptor-ligands-in-seizure-models-in-vivo
#17
Edijs Vavers, Baiba Svalbe, Lasma Lauberte, Ilmars Stonans, Ilga Misane, Maija Dambrova, Liga Zvejniece
Sigma-1 receptor (Sig1R) is a ligand-regulated protein which, since its discovery, has been widely studied as a novel target to treat neurological disorders, including seizures. However, the roles and mechanisms of Sig1R in the regulation of seizures are not fully understood. The aim of the present study was to test and compare effects of often used selective Sig1R ligands in models of experimentally induced seizures. The anti-seizure activities and interactions of selective Sig1R agonist PRE-084, selective Sig1R antagonist NE-100 and novel positive allosteric Sig1R modulator E1R were evaluated in pentylenetetrazol (PTZ) and (+)-bicuculline (BIC)-induced seizure models in mice...
April 4, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28386653/cell-viability-and-hemocompatibility-evaluation-of-a-starch-based-hydrogel-loaded-with-hydroxyapatite-or-calcium-carbonate-for-maxillofacial-bone-regeneration
#18
Juan Carlos Flores-Arriaga, Amaury de Jesús Pozos-Guillén, Diana María Escobar-García, Christian Grandfils, Bernardino Isaac Cerda-Cristerna
The objective of this study is to evaluate the cell viability and hemocompatibility of starch-based hydrogels for maxillofacial bone regeneration. Seven starch-based hydrogels were prepared: three loaded with 0.5, 1 and 2% calcium carbonate (Sigma Aldrich, St. Louis, MO, USA); three loaded with 2, 3 and 4% hydroxyapatite (Sigma Aldrich); and one not loaded as a control. A 10 M NaOH was then added to induce hydrogel formation. Human osteoblasts were cultured on each hydrogel for 72 h. An MTS assay (Cell Titer96; PROMEGA, Madison, WI, USA) was used to assess cell viability...
April 6, 2017: Odontology
https://www.readbyqxmd.com/read/28385503/novel-small-molecule-guanidine-sigma1-inhibitors-for-advanced-prostate-cancer
#19
Joseph M Salvino, Yellamelli V V Srikanth, Rongliang Lou, Halley M Oyer, Nan Chen, Felix J Kim
Prostate cancer is the most frequently diagnosed malignancy and the leading cause of cancer related death in men. First line therapy for disseminated disease relies on androgen deprivation, leveraging the addiction of these tumors on androgens for both growth and survival. Treatment typically involves antagonizing the androgen receptor (AR) or blocking the synthesis of androgens. Recurrence is common and within 2-3years patients develop castration resistant tumors that become unresponsive to AR-axis targeted therapies...
March 18, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28384850/application-of-sigma-metrics-and-performance-comparison-between-two-biochemistry-analyser-and-a-blood-gas-analyser-for-the-determination-of-electrolytes
#20
Yasemin Ustundag-Budak, Kagan Huysal
INTRODUCTION: Electrolytes have a narrow range of biological variation and small changes are clinically significant. It is important to select the best method for clinical decision making and patient monitoring in the emergency room. The sigma metrics model provides an objective method to evaluate the performance of a method. AIM: To calculate sigma metrics for electrolytes measured with one arterial blood gas analyser including two auto-analysers that use different technologies...
February 2017: Journal of Clinical and Diagnostic Research: JCDR
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