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https://www.readbyqxmd.com/read/29055045/diagnostic-relevance-of-ige-sensitization-profiles-to-eight-recombinant-phleum-pratense-molecules
#1
Francesca Cipriani, Carla Mastrorilli, Salvatore Tripodi, Giampaolo Ricci, Serena Perna, Valentina Panetta, Riccardo Asero, Arianna Dondi, Annamaria Bianchi, Nunzia Maiello, Michele Miraglia Del Giudice, Tullio Frediani, Francesco Macrì, Sandra Lucarelli, Iride Dello Iacono, Maria Francesca Patria, Elena Varin, Diego Peroni, Loredana Chini, Viviana Moschese, Roberto Bernardini, Giuseppe Pingitore, Umberto Pelosi, Mariangela Tosca, Francesco Paravati, Ifigenia Sfika, Andrea Di Rienzo Businco, Calotta Povesi Dascola, Pasquale Comberiati, Simone Frediani, Caterina Lambiase, Maria Carmen Verga, Diego Faggian, Mario Plebani, Mauro Calvani, Carlo Caffarelli, Paolo Maria Matricardi
BACKGROUND: Grass pollen-related seasonal allergic rhinoconjunctivitis (SARg) is clinically heterogeneous in severity, comorbidities and response to treatment. The component-resolved diagnostics disclosed also a high heterogeneity at molecular level. Our study aimed at analyzing the characteristics of the IgE sensitization to Phleum pratense molecules and investigating the diagnostic relevance of such molecules in childhood. METHODS: We examined 1120 children (age 4-18y) with SARg...
October 20, 2017: Allergy
https://www.readbyqxmd.com/read/29054090/diopside-magnetite-a-novel-nanocomposite-for-hyperthermia-applications
#2
Majid Abdellahi, Ebrahim Karamian, Aliakbar Najafinezhad, Fatemah Ranjabar, Akbar Chami, Amirsalar Khandan
In the present work, the releasing heat, scaffold apatite formation, and magnetic behavior of a novel diopside-magnetite nanocomposite with various contents of magnetite (Fe3O4) were evaluated. The N´eel and Brown relaxations did not have a significant effect on the specific absorption rate (SAR) of the composite samples. Indeed, magnetic saturation, Ms, indicated a crucial effect on the heat release of the samples. The sample with 30wt% magnetite had the highest value of SAR, while the sample with 20wt% magnetite, in the form of scaffold, allowed the high amount of apatite formation on its surface...
October 9, 2017: Journal of the Mechanical Behavior of Biomedical Materials
https://www.readbyqxmd.com/read/29052924/mers-sars-and-other-coronaviruses-as-causes-of-pneumonia
#3
REVIEW
Yudong Yin, Richard G Wunderink
Human coronaviruses (HCoVs) have been considered to be relatively harmless respiratory pathogens in the past. However, after the outbreak of the severe acute respiratory syndrome (SARS) and emergence of the Middle East respiratory syndrome (MERS), HCoVs have received worldwide attention as important pathogens in respiratory tract infection. This review focuses on the epidemiology, pathogenesis and clinical characteristics among SARS-coronaviruses (CoV), MERS-CoV and other HCoV infections.
October 20, 2017: Respirology: Official Journal of the Asian Pacific Society of Respirology
https://www.readbyqxmd.com/read/29050781/examination-of-%C3%AE-exosite-inhibitors-against-botulinum-neurotoxin-a-protease-through-structure-activity-relationship-studies-of-chicoric-acid
#4
Song Xue, Hajime Seki, Marek Remes, Peter Šilhár, Kim Janda
Botulinum neurotoxins (BoNT) are among the most toxic known substances and currently there are no effective treatments for intraneuronal BoNT intoxication. Chicoric acid (ChA) was previously reported as a BoNT/A inhibitor that binds to the enzyme's α-exosite. Herein, we report the synthesis and structure-activity relationships (SARs) of a series of ChA derivatives, which revealed essential binding interactions between ChA and BoNT/A. Moreover, several ChA-based inhibitors with improved potency against the BoNT/A were discovered...
October 12, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29048389/discovery-of-novel-n-substituted-prolinamido-indazoles-as-potent-rho-kinase-inhibitors-and-vasorelaxation-agents
#5
Yangyang Yao, Renze Li, Xiaoyu Liu, Feilong Yang, Ying Yang, Xiaoyu Li, Xiang Shi, Tianyi Yuan, Lianhua Fang, Guanhua Du, Xiaozhen Jiao, Ping Xie
Inhibitors of Rho kinase (ROCK) have potential therapeutic applicability in a wide range of diseases, such as hypertension, stroke, asthma and glaucoma. In a previous article, we described the lead discovery of DL0805, a new ROCK I inhibitor, showing potent inhibitory activity (IC50 6.7 μM). Herein, we present the lead optimization of compound DL0805, resulting in the discovery of 24- and 39-fold more-active analogues 4a (IC50 0.27 μM) and 4b (IC50 0.17 μM), among other active analogues. Moreover, ex-vivo studies demonstrated that 4a and 4b exhibited comparable vasorelaxant activity to the approved drug fasudil in rat aortic rings...
October 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29046686/combining-fungicides-and-prospective-npr1-based-just-in-time-immunomodulating-chemistries-for-crop-protection
#6
Xiahezi Kuai, Charles Barraco, Charles Després
Each year, crop yield is lost to weeds competing for resources, insect herbivory and diseases caused by pathogens. To thwart these insults and preserve yield security and a high quality of traits, conventional agriculture makes use of improved cultivars combined with fertilizer and agrochemical applications. However, given that regulatory bodies and consumers are demanding environmentally safer agrochemicals, while at the same time resistance to agrochemicals is mounting, it is crucial to adopt a "holistic" approach to agriculture by not excluding any number of management tools at our disposal...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/29046679/overexpression-of-npr1-in-brassica-juncea-confers-broad-spectrum-resistance-to-fungal-pathogens
#7
Sajad Ali, Zahoor A Mir, Anshika Tyagi, Hailay Mehari, Rajendra P Meena, Javaid A Bhat, Prashant Yadav, Pradeep Papalou, Sandhya Rawat, Anita Grover
Brassica juncea (Indian mustard) is a commercially important oil seed crop, which is highly affected by many biotic stresses. Among them, Alternaria leaf blight and powdery mildew are the most devastating diseases leading to huge yield losses in B. juncea around the world. In this regard, genetic engineering is a promising tool that may possibly allow us to enhance the B. juncea disease resistance against these pathogens. NPR1 (non-expressor of pathogen-related gene 1) is a bonafide receptor of salicylic acid (SA) which modulates multiple immune responses in plants especially activation of induced and systemic acquired resistance (SAR)...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/29045446/changes-in-numbers-and-size-of-synaptic-vesicles-of-cortical-neurons-induced-by-exposure-to-835-mhz-radiofrequency-electromagnetic-field
#8
Ju Hwan Kim, Hyo-Jeong Kim, Da-Hyeon Yu, Hee-Seok Kweon, Yang Hoon Huh, Hak Rim Kim
We studied the effects of radiofrequency electromagnetic fields (RF-EMFs) exposure on neuronal functions of mice. Particularly, we focused on RF-EMF effects on synaptic vesicles (SVs), which store neurotransmitters at axon terminals or synaptic boutons. C57 BL/6 mice were exposed to 835 MHz RF-EMF (4.0 W/kg SAR, for 5 h daily) and alterations in SVs at presynaptic terminals in the cerebral cortex were determined. Ultrastructure of randomly selected cortical neurons was observed using typical electron microscopy and bio-high voltage electron microscopy (Bio-HVEM) methods, which enable the estimation of the numbers and size of SVs...
2017: PloS One
https://www.readbyqxmd.com/read/29044748/assembly-of-coordination-polymers-using-thioether-functionalized-octasilsesquioxanes-occurrence-of-cux-n-clusters-x-br-and-i-within-3d-poss-networks
#9
Abhinav Raghuvanshi, Carsten Strohmann, Jean-Baptiste Tissot, Sébastien Clément, Ahmad Mehdi, Sébastien Richeter, Lydie Viau, Michael Knorr
For the first time, POSS-based coordination polymers (CPs) have been structurally characterized. These CPs were obtained in high yield via self-assembly reactions of thioether-functionalized polysilsesquioxanes with Cu(I) salts under mild conditions. Single-crystal analyses revealed the formation of 3D networks incorporating different secondary building units (SBUs) as connection nodes. The nature of the -SAr function allows a fine-tuning of the cluster nuclearity, i.e. butterfly-shaped Cu2X2 or closed cubane-type Cu4I4 cores...
October 18, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29040655/effects-of-1950-mhz-radiofrequency-electromagnetic-fields-on-a%C3%AE-processing-in-human-neuroblastoma-and-mouse-hippocampal-neuronal-cells
#10
Jeongyeon Park, Jong Hwa Kwon, Nam Kim, Kiwon Song
Alzheimer's disease (AD) is a neurodegenerative disease leading to progressive loss of memory and other cognitive functions. One of the well-known pathological markers of AD is the accumulation of amyloid-beta protein (Aβ), and its plaques, in the brain. Recent studies using Tg-5XFAD mice as a model of AD have reported that exposure to radiofrequency electromagnetic fields (RF-EMF) from cellular phones reduced Aβ plaques in the brain and showed beneficial effects on AD. In this study, we examined whether exposure to 1950 MHz RF-EMF affects Aβ processing in neural cells...
October 6, 2017: Journal of Radiation Research
https://www.readbyqxmd.com/read/29039760/sea-cucumber-glycosides-chemical-structures-producing-species-and-important-biological-properties
#11
REVIEW
Muhammad Abdul Mojid Mondol, Hee Jae Shin, M Aminur Rahman, Mohamad Tofazzal Islam
Sea cucumbers belonging to echinoderm are traditionally used as tonic food in China and other Asian countries. They produce abundant biologically active triterpene glycosides. More than 300 triterpene glycosides have been isolated and characterized from various species of sea cucumbers, which are classified as holostane and nonholostane depending on the presence or absence of a specific structural unit γ(18,20)-lactone in the aglycone. Triterpene glycosides contain a carbohydrate chain up to six monosaccharide units mainly consisting of d-xylose, 3-O-methy-d-xylose, d-glucose, 3-O-methyl-d-glucose, and d-quinovose...
October 17, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29038479/probing-ligand-recognition-of-the-opioid-pan-antagonist-at-076-at-nociceptin-kappa-mu-and-delta-opioid-receptors-through-structure-activity-relationships
#12
V Blair Journigan, Willma E Polgar, Edward W Tuan, James Lu, Pankaj R Daga, Nurulain T Zaveri
Few opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high affinity at the fourth opioid receptor, the nociceptin/orphanin FQ receptor (NOP). We recently reported the discovery of AT-076 (1), (R)-7-hydroxy-N-((S)-1-(4-(3-hydroxyphenyl)piperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity for all four subtypes. Since AT-076 binds with high affinity at all four subtypes, we conducted a structure-activity relationship (SAR) study to probe ligand recognition features important for pan opioid receptor activity, using chemical modifications of key pharmacophoric groups...
October 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29038364/oral-and-intravenous-pharmacokinetics-of-taurine-in-sprague-dawley-rats-the-influence-of-dose-and-the-possible-involvement-of-the-proton-coupled-amino-acid-transporter-pat1-in-oral-taurine-absorption
#13
Carsten Uhd Nielsen, Maria Bjerg, Nithiya Ulaganathan, René Holm
Taurine is involved in various physiological processes, and one of the most abundant amino acids in human. The aim was to investigate the mechanism for intestinal absorption of taurine in vivo using also in vitro mechanistic studies. Taurine absorption was measured in male Sprague-Dawley rats at 10-997 mg/kg and 1-30 mg/kg for oral and intravenous administration, respectively. Oral absorption was measured in the presence of substrates for the proton-coupled amino acid transporter, PAT1, that is, 200 mg/kg proline (Pro) and sarcosine (Sar), and in the presence of 2-Amino-2-norbornanecarboxylic acid (BCH) (200 mg/kg)...
October 2017: Physiological Reports
https://www.readbyqxmd.com/read/29038024/structural-insights-of-a-self-assembling-9-residue-peptide-from-the-c-terminal-tail-of-the-sars-corona-virus-e-protein-in-dpc-and-sds-micelles-a-combined-high-and-low-resolution-spectroscopic-study
#14
Anirban Ghosh, Dipita Bhattacharyya, Anirban Bhunia
In recent years, several studies based on the interaction of self-assembling short peptides derived from Viroporins with model membranes, have improved our understanding of the molecular mechanism of Corona virus (CoV) infection under physiological conditions. In this study, we have characterized the mechanism of membrane interaction of a short, 9-residue peptide TK9 (T(55)VYVYSRVK(63)) that had been derived from the carboxyl terminal of the Severe Acute Respiratory Syndrome (SARS) Corona virus (SARS CoV) Envelope (E) protein...
October 13, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29036058/nonrigid-synthetic-aperture-radar-and-optical-image-coregistration-by-combining-local-rigid-transformations-using-a-kohonen-network
#15
Mehdi Salehpour, Alireza Behrad
This study proposes a new algorithm for nonrigid coregistration of synthetic aperture radar (SAR) and optical images. The proposed algorithm employs point features extracted by the binary robust invariant scalable keypoints algorithm and a new method called weighted bidirectional matching for initial correspondence. To refine false matches, we assume that the transformation between SAR and optical images is locally rigid. This property is used to refine false matches by assigning scores to matched pairs and clustering local rigid transformations using a two-layer Kohonen network...
October 1, 2017: Journal of the Optical Society of America. A, Optics, Image Science, and Vision
https://www.readbyqxmd.com/read/29035537/discovery-of-a-novel-piperidine-based-inhibitor-of-cholesteryl-ester-transfer-protein-cetp-that-retains-activity-in-hypertriglyceridemic-plasma
#16
Ken Yamada, Margaret Brousseau, Wataru Honma, Akiko Iimura, Hidetomo Imase, Yuki Iwaki, Toshio Kawanami, Daniel LaSala, Guiqing Liang, Hironobu Mitani, Kazuhiko Nonomura, Osamu Ohmori, Meihui Pan, Dean F Rigel, Ichiro Umemura, Kayo Yasoshima, Guoming Zhu, Muneto Mogi
Herein we describe the discovery and characterization of a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP) with a core structure distinct from other reported CETP inhibitors. A versatile synthesis starting from 4-methoxypyridine enabled an efficient exploration of the SAR, giving a lead molecule with potent CETP inhibition in human plasma. The subsequent optimization focused on improvement of pharmacokinetics and mitigation of off-target liabilities, such as CYP inhibition, whose improvement correlated with increased lipophilic efficiency...
October 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29035208/an-efficient-integral-based-method-for-three-dimensional-mr-ept-and-the-calculation-of-the-rf-coil-induced-field
#17
Lei Guo, Jin Jin, Chunyi Liu, Feng Liu, Stuart Crozier
Magnetic resonance electrical property tomography (MR-EPT) has significant potential for the estimation of the electrical properties (EPs) of tissue, which are essential for the calculation of specific absorption rates (SAR), a critical safety factor requiring monitoring and controlling in applications of ultra-high field magnetic resonance imaging (MRI). In this paper, a novel, efficient method based on integral equations is proposed for the calculation of the EPs and the RF-coil induced field. An inverse problem framework is first constructed to include the forward problem operator, while the EPs are reconstructed by using a non-linear conjugate gradient method (NLCG)...
October 16, 2017: IEEE Transactions on Bio-medical Engineering
https://www.readbyqxmd.com/read/29034580/selective-inhibition-of-trpm2-channel-by-two-novel-synthesized-adpr-analogues
#18
Xiao Luo, Meng Li, Kaiyu Zhan, Wei Yang, Lihe Zhang, KeWei Wang, Peilin Yu, Liangren Zhang
Transient receptor potential melastatin-2 (TRPM2) channel critical for monitoring internal body temperature is implicated in the pathological processes such as neurodegeneration. However, lacking selective and potent TRPM2 inhibitors impedes investigation and validation of the channel as a drug target. To discover novel and selective TRPM2 inhibitors, a series of adenosine 5'-diphosphoribose (ADPR) analogues were synthesized and their activities and selectivity were evaluated. Whole-cell patch clamp recordings were employed for screen and evaluation of synthesized compounds...
October 15, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29034465/gene-expression-tradeoffs-between-defence-and-growth-in-english-elm-induced-by-ophiostoma-novo-ulmi
#19
Pedro Perdiguero, Juan Sobrino-Plata, Martin Venturas, Juan Antonio Martín, Luis Gil, Carmen Collada
Wilt diseases caused by vascular pathogens include some of the most damaging stresses affecting trees. Dutch elm disease (DED), caused by the fungus Ophiostoma novo-ulmi, destroyed most of North American and European elm populations in the 20th century. The highly susceptible English elm, also known as Atinian clone, suffered the highest mortality rates during the last pandemic event, probably due to its lack of genetic diversity. To study the DED pathosystem, we inoculated English elm ramets with O. novo-ulmi and evaluated xylem anatomy, molecular response and disease symptoms...
October 15, 2017: Plant, Cell & Environment
https://www.readbyqxmd.com/read/29034069/scaffold-hopping-via-anchor-query-%C3%AE-lactams-as-potent-p53-mdm2-antagonists-%C3%A2
#20
S Shaabani, C G Neochoritis, A Twarda-Clapa, B Musielak, T A Holak, A Dömling
Using the pharmacophore-based virtual screening platform ANCHOR.QUERY, we morphed our recently described Ugi-4CR scaffold towards a β-lactam scaffold with potent p53-MDM2 antagonizing activities. 2D-HSQC and FP measurements confirm potent MDM2 binding. Molecular modeling studies are used to understand the observed SAR in the β-lactam series.
May 1, 2017: MedChemComm
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