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https://www.readbyqxmd.com/read/27933730/reactivity-of-9-aminoacridine-drug-quinacrine-with-glutathione-limits-its-anti-prion-activity
#1
Martin Šafařík, Tibor Moško, Zbigniew Zawada, Eva Šafaříková, Martin Dračínský, Karel Holada, Jaroslav Šebestík
Quinacrine - the drug based on 9-aminoacridine - failed in clinical trials for prion diseases, whereas it was active in in-vitro studies. We hypothesize that aromatic nucleophilic substitution at C9 could be contributing factor responsible for this failure because of the transfer of acridine moiety from quinacrine to abundant glutathione. Here, we described the semi-large-scale synthesis of the acridinylated glutathione and the consequences of its formation on biological and biophysical activities. The acridinylated glutathione is one order of magnitude weaker prion protein binder than the parent quinacrine...
December 9, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27933673/a-biophysical-and-computational-study-unraveling-the-molecular-interaction-mechanism-of-a-new-janus-kinase-inhibitor-tofacitinib-with-bovine-serum-albumin
#2
Ali Saber Abdelhameed, Saima Nusrat, Mohammad Rehan Ajmal, Syed Mohammad Zakariya, Masihuz Zaman, Rizwan Hasan Khan
The interaction of a recently certified kinase inhibitor Tofacitinib (TFB) with bovine serum albumin (BSA) has been studied, by spectroscopic and molecular docking studies. Spectrofluorimetric measurements at 3 different temperatures (288, 298, and 310 K) showed that TFB quench the intrinsic fluorescence of BSA upon forming a nonfluorescent complex. The intrinsic fluorescence data showed that TFB binds to BSA with binding constant (Kb ) of approximately 10(4) M(-1) , affirming a significant affinity of TFB with BSA...
December 9, 2016: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/27933654/in-vitro-detection-of-diesel-exhaust-particles-induced-human-lung-carcinoma-epithelial-cells-damage-and-the-effect-of-resveratrol
#3
Qifei Li, Mingjie Tang, Anhong Zhou
People are taking up antioxidants in their daily diet and being exposed to a potential diesel exhaust particles (DEP)-containing environment. Thus it is important to study in vitro cellular responses when cells are exposed to DEP with or without antioxidant treatment. The investigation of DEP and resveratrol (RES) on cellular biophysical and biochemical changes is needed to better understand the mechanisms of DEP and RES in mammalian cells. A combination of two non-invasive techniques (atomic force microscopy, AFM, and Raman spectroscopy, RM) and multimodal tools were applied to evaluate the biophysical, biochemical alterations and cytokine, membrane potential and cell cycle of cells with or without RES pretreatment to different times of DEP exposure...
December 9, 2016: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/27933577/environmental-and-health-impacts-of-effluents-from-textile-industries-in-ethiopia-the-case-of-gelan-and-dukem-oromia-regional-state
#4
Diriba Dadi, Till Stellmacher, Feyera Senbeta, Steven Van Passel, Hossein Azadi
This study focuses on four textile industries (DH-GEDA, NOYA, ALMHADI, and ALSAR) established between 2005 and 2008 in the peri-urban areas of Dukem and Gelan. The objectives of the study were to generate baseline information regarding the concentration levels of selected pollutants and to analyze their effects on biophysical environments. This study also attempts to explore the level of exposure that humans and livestock have to polluted effluents and the effects thereof. The findings of this study are based on data empirically collected from two sources: laboratory analysis of sample effluents from the four selected textile plants and quantitative as well as qualitative socioeconomic data collection...
January 2017: Environmental Monitoring and Assessment
https://www.readbyqxmd.com/read/27933406/differential-roles-for-the-coagulation-factors-xi-and-xii-in-regulating-the-physical-biology-of-fibrin
#5
Joanna L Sylman, Uranbileg Daalkhaijav, Ying Zhang, Elliot M Gray, Parsa A Farhang, Tiffany T Chu, Jevgenia Zilberman-Rudenko, Cristina Puy, Erik I Tucker, Stephanie A Smith, James H Morrissey, Travis W Walker, Xiaolin L Nan, András Gruber, Owen J T McCarty
In the contact activation pathway of the coagulation, zymogen factor XII (FXII) is converted to FXIIa, which triggers activation of FXI leading to the activation of FIX and subsequent thrombin generation and fibrin formation. Feedback activation of FXI by thrombin has been shown to promote thrombin generation in a FXII-independent manner and FXIIa can bypass FXI to directly activate FX and prothrombin in the presence of highly negatively charged molecules, such as long-chain polyphosphates (LC polyP). We sought to determine whether activation of FXII or FXI differentially regulate the physical biology of fibrin formation...
December 8, 2016: Annals of Biomedical Engineering
https://www.readbyqxmd.com/read/27933246/a-quantitative-report-on-the-impact-of-chloride-on-the-kinetic-coefficients-of-auxin-induced-growth-a-numerical-contribution-to-the-acid-growth-hypothesis
#6
Mariusz Pietruszka, Aleksandra Haduch-Sendecka
This work presents the application of several our own novel methods of analysing the kinetics of plant growth, which create, among others, a common platform for the comparison of experimental results. A relatively simple formula is used to parameterize the wide range of data that has been obtained for Zea mays L. in the literature, though it can also be used for different species. A biophysical/biochemical interpretation of the parameters was obtained from a theoretical model that is based on a modified Lockhart equation...
2016: SpringerPlus
https://www.readbyqxmd.com/read/27932457/structural-basis-for-the-dimerization-of-nab2-generated-by-rna-binding-provides-insight-into-its-contribution-to-both-poly-a-tail-length-determination-and-transcript-compaction-in-saccharomyces-cerevisiae
#7
Shintaro Aibara, James M B Gordon, Anja S Riesterer, Stephen H McLaughlin, Murray Stewart
In Saccharomyces cerevisiae generation of export-competent mRNPs terminates the nuclear phase of the gene expression pathway and facilitates transport to the cytoplasm for translation. Nab2 functions in this process to control both mRNP compaction that facilitates movement through nuclear pore complexes and the length of transcript poly(A) tails. Nab2 has a modular structure that includes seven CCCH Zn fingers that bind to A-rich RNAs and fingers 5-7 are critical for these functions. Here, we demonstrate, using both biophysical and structural methods, that binding A11G RNA induces dimerization of Zn fingers 5-7 mediated by the novel spatial arrangement of the fingers promoting each RNA chain binding two protein chains...
December 8, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27932294/large-scale-structure-based-prediction-and-identification-of-novel-protease-substrates-using-computational-protein-design
#8
Manasi A Pethe, Aliza B Rubenstein, Sagar D Khare
Characterizing the substrate specificity of protease enzymes is critical for illuminating the molecular basis of their diverse and complex roles in a wide array of biological processes. Rapid and accurate prediction of their extended substrate specificity would also aid in the design of custom proteases capable of selectively and controllably cleaving biotechnologically or therapeutically relevant targets. However, current in silico approaches for protease specificity prediction, rely on, and are therefore limited by, machine learning of sequence patterns in known experimental data...
December 5, 2016: Journal of Molecular Biology
https://www.readbyqxmd.com/read/27932256/a-panorama-of-bacterial-inulinases-production-purification-characterization-and-industrial-applications
#9
REVIEW
Ram Sarup Singh, Kanika Chauhan, John F Kennedy
Inulinases are important hydrolysing enzymes which specifically act on β-2, 1 linkages of inulin to produce fructose or fructooligosaccharides. Fungi, yeasts and bacteria are the potent microbial sources of inulinases. The data on bacterial inulinases is scarce as compared to other microbial sources. Inulinases yield from bacteria is very less as compared to fungal and yeast sources of inulinases. Submerged fermentation (SmF) is the method of choice for the production of inulinases from bacterial sources. Moreover, inulin is a potent substrate for the production of inulinases in SmF...
December 5, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27932064/bax-and-bak-pores-are-we-closing-the-circle
#10
REVIEW
Katia Cosentino, Ana J García-Sáez
Bax and its homolog Bak are key regulators of the mitochondrial pathway of apoptosis. On cell stress Bax and Bak accumulate at distinct foci on the mitochondrial surface where they undergo a conformational change, oligomerize, and mediate cytochrome c release, leading to cell death. The molecular mechanisms of Bax and Bak assembly and mitochondrial permeabilization have remained a longstanding question in the field. Recent structural and biophysical studies at several length scales have shed light on key aspects of Bax and Bak function that have shifted how we think this process occurs...
December 5, 2016: Trends in Cell Biology
https://www.readbyqxmd.com/read/27930818/pyridine-nucleotide-transhydrogenase-pntab-is-essential-for-optimal-growth-and-photosynthetic-integrity-under-low-light-mixotrophic-conditions-in-synechocystis-sp-pcc-6803
#11
Jari Kämäräinen, Tuomas Huokko, Sanna Kreula, Patrik R Jones, Eva-Mari Aro, Pauli Kallio
Pyridine nucleotide transhydrogenase (PntAB) is an integral membrane protein complex participating in the regulation of NAD(P)(+) :NAD(P)H redox homeostasis in various prokaryotic and eukaryotic organisms. In the present study we addressed the function and biological role of PntAB in oxygenic photosynthetic cyanobacteria capable of both autotrophic and heterotrophic growth, with support from structural three-dimensional (3D)-modeling. The pntA gene encoding the α subunit of heteromultimeric PntAB in Synechocystis sp...
December 8, 2016: New Phytologist
https://www.readbyqxmd.com/read/27930673/dopamine-neurons-change-the-type-of-excitability-in-response-to-stimuli
#12
Ekaterina O Morozova, Denis Zakharov, Boris S Gutkin, Christopher C Lapish, Alexey Kuznetsov
The dynamics of neuronal excitability determine the neuron's response to stimuli, its synchronization and resonance properties and, ultimately, the computations it performs in the brain. We investigated the dynamical mechanisms underlying the excitability type of dopamine (DA) neurons, using a conductance-based biophysical model, and its regulation by intrinsic and synaptic currents. Calibrating the model to reproduce low frequency tonic firing results in N-methyl-D-aspartate (NMDA) excitation balanced by γ-Aminobutyric acid (GABA)-mediated inhibition and leads to type I excitable behavior characterized by a continuous decrease in firing frequency in response to hyperpolarizing currents...
December 2016: PLoS Computational Biology
https://www.readbyqxmd.com/read/27929189/switching-substitution-groups-on-the-in-tether-chiral-centre-influences-backbone-peptides-permeability-and-target-binding-affinity
#13
Yixiang Jiang, Kuan Hu, Xiaodong Shi, Qingzhuang Tang, ZiChen Wang, Xiyang Ye, Zigang Li
Different substitution groups on the in-tether chiral centre of chirality-induced helical peptides (CIH peptides) showed distinguishable effects on the peptides' cellular uptakes and binding affinities with the estrogen receptor α(ER-α). This study proves that in-tether chiral centres are a valuable modification site for constructing peptide ligands with preferable biophysical properties.
December 8, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27928907/separation-of-hiv-1-gag-virus-like-particles-from-vesicular-particles-impurities-by-hydroxyl-functionalized-monoliths
#14
Petra Steppert, Daniel Burgstaller, Miriam Klausberger, Petra Kramberger, Andres Tover, Eva Berger, Katharina Nöbauer, Ebrahim Razzazi-Fazeli, Alois Jungbauer
The downstream processing of enveloped virus-like particles is very challenging because of the biophysical and structural similarity between correctly assembled particles and contaminating vesicular particles present in the feedstock. We used hydroxyl-functionalized polymethacrylate monoliths, providing hydrophobic and electrostatic binding contributions, for the purification of HIV-1 gag virus-like particles. The clarified culture supernatant was conditioned with ammonium sulfate and after membrane filtration, loaded onto a 1 mL monolith...
December 8, 2016: Journal of Separation Science
https://www.readbyqxmd.com/read/27928710/synthesis-characterization-and-bioactivity-studies-of-novel-1-3-4-oxadiazole-small-molecule-that-targets-basic-phospholipase-a2-from-vipera-russelli
#15
Vivek Hamse Kameshwar, Kumar J R, Babu S Priya, S Nanjunda Swamy
Secretory phospholipase A2 (sPLA2) is a key enzyme participating in the inflammatory cascade followed by the action of cyclooxygenase-2 and lipoxygenases. Therefore, inhibitors of sPLA2 could be used as potent anti-inflammatory agents to treat the early phase of inflammation. In this study, we have prepared the fenoprofen and ibuprofen analogs containing 1,3,4-oxadiazole nucleus and tested against Vipera russelli venom's basic sPLA2 (VRV-PL-VIIIa). Among the tested ligands 5(a-t),2-(2-chlorophenyl)-5-(1-(4-phenoxyphenyl) ethyl)-1,3,4-oxadiazole (5m) inhibited the catalytic activity of VRV-PL-VIIIa with an IC50 value of 11...
December 7, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27927232/publication-of-nuclear-magnetic-resonance-experimental-data-with-semantic-web-technology-and-the-application-thereof-to-biomedical-research-of-proteins
#16
Masashi Yokochi, Naohiro Kobayashi, Eldon L Ulrich, Akira R Kinjo, Takeshi Iwata, Yannis E Ioannidis, Miron Livny, John L Markley, Haruki Nakamura, Chojiro Kojima, Toshimichi Fujiwara
BACKGROUND: The nuclear magnetic resonance (NMR) spectroscopic data for biological macromolecules archived at the BioMagResBank (BMRB) provide a rich resource of biophysical information at atomic resolution. The NMR data archived in NMR-STAR ASCII format have been implemented in a relational database. However, it is still fairly difficult for users to retrieve data from the NMR-STAR files or the relational database in association with data from other biological databases. FINDINGS: To enhance the interoperability of the BMRB database, we present a full conversion of BMRB entries to two standard structured data formats, XML and RDF, as common open representations of the NMR-STAR data...
May 5, 2016: Journal of Biomedical Semantics
https://www.readbyqxmd.com/read/27927196/the-topology-structure-and-pe-interaction-of-litaf-underpin-a-charcot-marie-tooth-disease-type-1c
#17
Anita K Ho, Jane L Wagstaff, Paul T Manna, Lena Wartosch, Seema Qamar, Elspeth F Garman, Stefan M V Freund, Rhys C Roberts
BACKGROUND: Mutations in Lipopolysaccharide-induced tumour necrosis factor-α factor (LITAF) cause the autosomal dominant inherited peripheral neuropathy, Charcot-Marie-Tooth disease type 1C (CMT1C). LITAF encodes a 17 kDa protein containing an N-terminal proline-rich region followed by an evolutionarily-conserved C-terminal 'LITAF domain', which contains all reported CMT1C-associated pathogenic mutations. RESULTS: Here, we report the first structural characterisation of LITAF using biochemical, cell biological, biophysical and NMR spectroscopic approaches...
December 7, 2016: BMC Biology
https://www.readbyqxmd.com/read/27925669/biochemical-biophysical-and-cellular-techniques-to-study-the-guanine-nucleotide-exchange-factor-giv-girdin
#18
Pradipta Ghosh, Nicolas Aznar, Lee Swanson, I-Chung Lo, Inmaculada Lopez-Sanchez, Jason Ear, Cristina Rohena, Nicholas Kalogriopoulos, Linda Joosen, Ying Dunkel, Nina Sun, Peter Nguyen, Deepali Bhandari
Canonical signal transduction via heterotrimeric G proteins is spatiotemporally restricted, i.e., triggered exclusively at the plasma membrane, only by agonist activation of G protein-coupled receptors via a finite process that is terminated within a few hundred milliseconds. Recently, a rapidly emerging paradigm has revealed a noncanonical pathway for activation of heterotrimeric G proteins via the nonreceptor guanidine-nucleotide exchange factor, GIV/Girdin. Biochemical, biophysical, and functional studies evaluating this pathway have unraveled its unique properties and distinctive spatiotemporal features...
December 7, 2016: Current Protocols in Chemical Biology
https://www.readbyqxmd.com/read/27925328/screening-for-preeclampsia-in-the-first-trimester-the-usefulness-of-maternal-hemodynamics-and-bioimpedence-in-non-obese-patients
#19
Giulia Gagliardi, Grazia Maria Tiralongo, Damiano Lo Presti, Ilaria Pisani, Daniele Farsetti, Barbara Vasapollo, Gian Paolo Novelli, Angela Andreoli, Herbert Valensise
OBJECTIVE: To test if maternal hemodynamics, and bioimpedance, together with the Combined Screening (maternal history, biophysical and biochemical markers), are able to identify normotensive non-obese patients at risk for preeclampsia (PE) and/or intrauterine growth restriction (IUGR) in the first trimester of gestation. METHODS: 150 healthy nulliparous non-obese women (BMI<30Kg/m(2) ) were enrolled in the study in the first trimester of pregnancy and submitted to USCOM to detect hemodynamic parameters, bioimpedence to characterize body composition, and combined screening for preeclampsia (maternal history, biophysical and maternal biochemical markers)...
December 7, 2016: Ultrasound in Obstetrics & Gynecology
https://www.readbyqxmd.com/read/27925050/fetal-thrombotic-vasculopathy-a-case-report-and-literature-review
#20
Ana Berquo Peleja, Silvio Martinelli, Renata Lopes Ribeiro, Roberto Eduardo Bittar, Regina Schultz, Rossana Pulcineli Vieira Francisco
Introduction: Fetal thrombotic vasculopathy is a recently described placental alteration with varying degrees of involvement and often associated with adverse perinatal outcomes. The diagnosis is made histologically and therefore is postnatal, which makes it a challenge in clinical practice. Method: Case report and review of literature on the subject. Results: The present case refers to a pregnant woman presenting fetal growth restriction, with poor obstetrical past, and sent late to our service...
October 2016: Revista da Associação Médica Brasileira
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