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https://www.readbyqxmd.com/read/28528285/comparison-of-the-pharmacological-and-biological-properties-of-hpma-copolymer-pirarubicin-conjugates-a-single-chain-copolymer-conjugate-and-its-biodegradable-tandem-diblock-copolymer-conjugate
#1
Tomas Etrych, Kenji Tsukigawa, Hideaki Nakamura, Petr Chytil, Jun Fang, Karel Ulbrich, Masaki Otagiri, Hiroshi Maeda
In this study, we compared the enhanced permeability and retention (EPR) effect, toxicity, and therapeutic effect of the conjugate of the linear polymer poly(N-(2-hydroxypropyl)methacrylamide) (HPMA) with pirarubicin with an Mw below the renal threshold (39g/mol) (named LINEAR) and the disulfide-linked tandem-polymeric dimer of the poly(HPMA)-pirarubicin conjugate with an Mw above the renal threshold (93g/mol) (named DIBLOCK). The DIBLOCK conjugate, which was susceptible to reductive degradation, showed both a better EPR effect (tumor delivery) (2...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28528106/characterization-of-white-tea-metabolome-comparison-against-green-and-black-tea-by-a-nontargeted-metabolomics-approach
#2
Weidong Dai, Dongchao Xie, Meiling Lu, Pengliang Li, Haipeng Lv, Chen Yang, Qunhua Peng, Yin Zhu, Li Guo, Yue Zhang, Junfeng Tan, Zhi Lin
White tea is considered the least processed form of tea and is reported to have a series of potent bioactivities, such as antioxidant, anti-inflammatory, anti-mutagenic, and anti-cancer activities. However, the chemical composition of white tea and the dynamic changes of the metabolites during the manufacturing process are far from clear. In this study, we applied a nontargeted metabolomics approach based on ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF/MS) to comprehensively profile the characteristic metabolites of white tea...
June 2017: Food Research International
https://www.readbyqxmd.com/read/28528103/addition-of-exogenous-enzymes-to-diets-containing-grape-pomace-effects-on-intestinal-utilization-of-catechins-and-antioxidant-status-of-chickens
#3
S Chamorro, A Viveros, A Rebolé, I Arija, C Romero, I Alvarez, A Rey, A Brenes
Grape pomace (GP) is a rich source of polyphenols with antioxidant capacity. An experiment was conducted to study the effect of GP phenolic compounds included at 5 and 10%, and the addition (individually or combined) of hydrolyzing enzymes (carbohydrase enzyme complex and tannase at 500ppm) on intestinal utilization of catechins and antioxidant status in broiler chickens. A diet supplemented with 200ppm of α-tocopheryl acetate was also used. Our findings demonstrate the capacity of chickens to digest the monomeric (catechin, epicatechin, gallic acid, and epicatechin-O-gallate) and dimeric (procyanidin B1 and procyanidin B2) catechins present in grape pomace...
June 2017: Food Research International
https://www.readbyqxmd.com/read/28527430/bjerrum-pairs-in-ionic-solutions-a-poisson-boltzmann-approach
#4
Ram M Adar, Tomer Markovich, David Andelman
Ionic solutions are often regarded as fully dissociated ions dispersed in a polar solvent. While this picture holds for dilute solutions, at higher ionic concentrations, oppositely charged ions can associate into dimers, referred to as Bjerrum pairs. We consider the formation of such pairs within the nonlinear Poisson-Boltzmann framework and investigate their effects on bulk and interfacial properties of electrolytes. Our findings show that pairs can reduce the magnitude of the dielectric decrement of ionic solutions as the ionic concentration increases...
May 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28526885/experimental-linear-optics-simulation-of-ground-state-of-an-ising-spin-chain
#5
Peng Xue, Xian Zhan, Zhihao Bian
We experimentally demonstrate a photonic quantum simulator: by using a two-spin Ising chain (an isolated dimer) as an example, we encode the wavefunction of the ground state with a pair of entangled photons. The effect of magnetic fields, leading to a critical modification of the correlation between two spins, can be simulated by just local operations. With the ratio of simulated magnetic fields and coupling strength increasing, the ground state of the system changes from a product state to an entangled state and back to another product state...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526838/thioflavin-t-fluoresces-as-excimer-in-highly-concentrated-aqueous-solutions-and-as-monomer-being-incorporated-in-amyloid-fibrils
#6
Anna I Sulatskaya, Andrey V Lavysh, Alexander A Maskevich, Irina M Kuznetsova, Konstantin K Turoverov
Fluorescence of thioflavin T (ThT) is a proven tool for amyloid fibrils study. The correct model of ThT binding to fibrils is crucial to clarify amyloid fibrils structure and mechanism of their formation. Although there are convincing evidences that ThT has molecular rotor nature, implying it's binding to fibrils in monomer form, speculations concerning ThT binding to fibrils in aggregated forms appear in literature so far. The elaborated approach for fluorescence intensity correction on the inner filter effects applied to ThT aqueous solutions with a wide range of concentration allowed characterizing ThT excimers fluorescence and showing its difference from that of ThT bound to fibrils...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526714/constans-imparts-dna-sequence-specificity-to-the-histone-fold-nf-yb-nf-yc-dimer
#7
Nerina Gnesutta, Roderick W Kumimoto, Swadhin Swain, Matteo Chiara, Chamindika Siriwardana, David Stephen Horner, Ben F Holt, Roberto Mantovani
NF-Y is a heterotrimeric transcription factor that binds CCAAT elements. The NF-Y trimer is composed of a Histone Fold Domain (HFD) dimer (NF-YB/NF-YC) and NF-YA, which confers DNA sequence-specificity. NF-YA shares a conserved domain with the CCT (CONSTANS, CONSTANS-LIKE, TOC1) proteins. We show that CONSTANS (CO/BBX1), a master flowering regulator, forms a trimer with Arabidopsis NF-YB2/NF-YC3 to efficiently bind the CORE element of the FT promoter. We term this complex NF-CO. Using saturation mutagenesis EMSAs and RNA-Seq profiling of co, nf-yb, and nf-yc mutants, we identify CCACA elements as the core NF-CO binding site...
May 19, 2017: Plant Cell
https://www.readbyqxmd.com/read/28526409/expression-and-purification-of-functional-pdgf-receptor-beta
#8
Qingbin Shang, Liang Zhao, Xiaojing Wang, Meimei Wang, Sen-Fang Sui, Li-Zhi Mi
Platelet Derived Growth Factor receptors (PDGFRs), members of receptor tyrosine kinase superfamily, play essential roles in early hematopoiesis, angiogenesis and organ development. Dysregulation of PDGF receptor signaling under pathological conditions associates with cancers, vascular diseases, and fibrotic diseases. Therefore, they are attractive targets in drug development. Like any other membrane proteins with a single-pass transmembrane domain, the high-resolution structural information of the full-length PDGF receptors is still not resolved...
May 16, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28526135/regulation-of-cell-calcium-and-role-of-plasma-membrane-calcium-atpases
#9
T Calì, M Brini, E Carafoli
The plasma membrane Ca(2+) ATPase (PMCA pump) is a member of the superfamily of P-type pumps. It has 10 transmembrane helices and 2 cytosolic loops, one of which contains the catalytic center. Its most distinctive feature is a C-terminal tail that contains most of the regulatory sites including that for calmodulin. The pump is also regulated by acidic phospholipids, kinases, a dimerization process, and numerous protein interactors. In mammals, four genes code for the four basic isoforms. Isoform complexity is increased by alternative splicing of primary transcripts...
2017: International Review of Cell and Molecular Biology
https://www.readbyqxmd.com/read/28525579/modulation-of-cyclobutane-thymine-photodimer-formation-in-t11-tracts-in-rotationally-phased-nucleosome-core-particles-and-dna-minicircles
#10
Kesai Wang, John-Stephen A Taylor
Cyclobutane pyrimidine dimers (CPDs) are DNA photoproducts linked to skin cancer, whose mutagenicity depends in part on their frequency of formation and deamination. Nucleosomes modulate CPD formation, favoring outside facing sites and disfavoring inward facing sites. A similar pattern of CPD formation in protein-free DNA loops suggests that DNA bending causes the modulation in nucleosomes. To systematically study the cause and effect of nucleosome structure on CPD formation and deamination, we have developed a circular permutation synthesis strategy for positioning a target sequence at different superhelix locations (SHLs) across a nucleosome in which the DNA has been rotationally phased with respect to the histone octamer by TG motifs...
May 19, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28525282/crowding-controlled-cluster-size-in-concentrated-aqueous-protein-solutions-structure-self-and-collective-diffusion
#11
Michal Katharina Braun, Marco Grimaldo, Felix Roosen-Runge, Ingo Hoffmann, Orsolya Czakkel, Michael Sztucki, Fajun Zhang, Frank Schreiber, Tilo Seydel
We investigate the concentration-controlled formation of clusters in β-lactoglobulin (BLG) protein solutions combining structural and dynamical scattering techniques. The static structure factor from small-angle X-ray scattering as well as de-Gennes narrowing in the nanosecond diffusion function D(q) from neutron spin echo spectroscopy support a picture of cluster formation. Using neutron backscattering spectroscopy, a monotonous increase of the average hydrodynamic cluster radius is monitored over a broad protein concentration range, corresponding to oligomeric structures of BLG ranging from the native dimers up to roughly four dimers...
May 19, 2017: Journal of Physical Chemistry Letters
https://www.readbyqxmd.com/read/28525272/direct-synthesis-of-an-unprecedented-stable-radical-of-nickel-ii-3-5-bis-dimedonyl-azadiisoindomethene-with-strong-and-narrow-near-infrared-absorption-at-%C3%AE-%C3%A2-1000-nm
#12
Elena A Makarova, Yuriy V Zatsikha, Kelly M E Newman, Vinod K Paidi, Valeria A Beletsky, Johan van Lierop, Evgeny A Lukyanets, Victor N Nemykin
An unprecedented stable neutral radical nickel(II) complex of 3,5-bis(dimedonyl)azadiisoindomethene (1) was prepared by the direct reaction between 1,3-diiminoisoindoline and dimedone. A new radical complex 1 has an intense and narrow absorption at 1008 nm and can be reduced to a less stable anionic [1](-) with a typical aza(dibenzo)boron dipyrromethene (aza-BODIPY) UV-vis spectrum. Complex 1, along with two other colored condensation reaction products 2 and 3, was characterized by spectroscopy and X-ray crystallography, while the paramagnetic nature of 1 was probed by EPR and SQUID methods...
May 19, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28525271/electron-spin-relaxation-and-biochemical-characterization-of-the-hydrogenase-maturase-hydf-insights-into-2fe-2s-and-4fe-4s-cluster-communication-and-hydrogenase-activation
#13
Eric M Shepard, Amanda S Byer, Priyanka Aggarwal, Jeremiah N Betz, Anna G Scott, Krista Shisler, Robert J Usselman, Gareth R Eaton, Sandra S Eaton, Joan B Broderick
Nature utilizes [FeFe]-hydrogenase enzymes to catalyze the interconversion between H2 and protons and electrons. Catalysis occurs at the H-cluster, a carbon monoxide, cyanide, and dithiomethylamine-coordinated 2Fe subcluster bridged via a cysteine to a [4Fe-4S] cluster. Biosynthesis of this unique metallocofactor is accomplished by three maturase enzymes denoted HydE, HydF, and HydG. HydE and HydG belong to the radical S-adenosylmethionine superfamily of enzymes and synthesize the nonprotein ligands of the H-cluster...
May 19, 2017: Biochemistry
https://www.readbyqxmd.com/read/28524768/anti-microrna-targeting-using-peptide-based-nanocomplexes-to-inhibit-differentiation-of-human-pancreatic-stellate-cells
#14
Jonas Schnittert, Praneeth R Kuninty, Tomasz F Bystry, Roland Brock, Gert Storm, Jai Prakash
AIM: To develop novel peptide-based nanocomplexes (NCs) for delivery of anti-miRNA oligonucleotides to human-derived pancreatic stellate cells (hPSCs), precursors of cancer-associated fibroblasts. MATERIALS & METHODS: NCs of anti-miRNA oligonucleotides and cell-penetrating peptides (different variants) were formed and characterized. The effects of anti-miR-199a delivery on hPSC differentiation and 3D heterospheroid formation were investigated. RESULTS: Dimeric cell-penetrating peptide based NCs (NC-2) showed 130-fold higher uptake by hPSCs compared with monomer-based NCs (NC-1) and tenfold higher uptake compared with general fibroblasts and different pancreatic tumor cells...
May 19, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28523927/retinoid-bms411-4-5-5-dimethyl-8-phenyl-5-6-dihydronaphthalen-2-yl-carbonyl-amino-benzoic-acid-a-potential-inhibitor-of-ns5a-protein-of-hepatitis-c-virus-a-candidate-for-combined-therapy-of-hepatitis-c-infection
#15
S Ibrahim, M J Asad, R T Mahmood, F H Wattoo, S Akhter, D Shahwar
Hepatitis C infection is a serious health issue worldwide caused by hepatitis C virus (HCV). There is an urgent need of search for new direct acting antiviral drugs due to the rapid development of drug resistance. The HCV NS5A protein is involved in creating resistance against antiviral therapy and there are also many reports that vitamin A deficiency is associated with non-responsiveness to antiviral treatment in HCV infected patients. So the present in silico study was aimed to find the relation between vitamin A deficiency and the NS5A protein's function in antiviral resistance...
2017: Acta Virologica
https://www.readbyqxmd.com/read/28523739/mechanisms-of-peptide-sex-pheromone-regulation-of-conjugation-in-enterococcus-faecalis
#16
Yuqing Chen, Arpan Bandyopadhyay, Briana K Kozlowicz, Heather A H Haemig, Albert Tai, Wei-Shou Hu, Gary M Dunny
In many gram positive bacteria, horizontal transfer and virulence are regulated by peptide-mediated cell-cell signaling. The heptapeptide cCF10 (C) activates conjugative transfer of the Enterococcus faecalis plasmid pCF10, whereas the iCF10 (I) peptide inhibits transfer. Both peptides bind to the same domain of the master transcription regulator PrgX, a repressor of transcription of the prgQ operon encoding conjugation genes. We show that repression of prgQ by PrgX tetramers requires formation of a pCF10 DNA loop where each of two PrgX DNA-binding sites is occupied by a dimer...
May 19, 2017: MicrobiologyOpen
https://www.readbyqxmd.com/read/28523647/computational-investigation-of-growth-hormone-receptor-trp169arg-heterozygous-mutation-in-a-child-with-short-stature
#17
William Farias Porto, Felipe Albuquerque Marques, Huri Brito Pogue, Maria Teresinha de Oliveira Cardoso, Maria Gabriela Rodrigues do Vale, Állan da Silva Pires, Octavio Luiz Franco, Sérgio Amorim de Alencar, Robert Pogue
Mutations in the growth hormone receptor (GHR) gene can cause disruption of the growth hormone signaling pathway, resulting in growth deficiency due to growth hormone (GH) resistance. Both recessive and apparently dominant mutations have been described in the literature. In order to shed some light on the molecular mechanism of partial growth hormone resistance caused by heterozygous mutations we performed an in-depth in silico analysis of a mutation found in a girl with a previous diagnosis of idiopathic short stature...
May 18, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28522883/in-situ-evaluation-of-estrogen-receptor-dimers-in-breast-carcinoma-cells-visualization-of-protein-protein-interactions
#18
Erina Iwabuchi, Yasuhiro Miki, Katsuhiko Ono, Yoshiaki Onodera, Hironobu Sasano
The estrogen receptor (ER) functions as a dimer and is involved in several different biological functions. However ER dimeric proteins have not been identified by in situ methodologies. Structured illumination microscopy (SIM) has been recently developed, which enabled the localization of protein and protein interaction. Therefore, in this study, we firstly demonstrated that ERs formed both homodimers and heterodimers in breast carcinoma cell lines using Nikon's SIM (N-SIM). ERα/α homodimers were detected in the nuclei of both ERα-positive MCF-7 and T-47D cells; 23...
April 27, 2017: Acta Histochemica et Cytochemica
https://www.readbyqxmd.com/read/28522847/a-molecular-basis-for-selective-antagonist-destabilization-of-dopamine-d3-receptor-quaternary-organization
#19
Sara Marsango, Gianluigi Caltabiano, Mireia Jiménez-Rosés, Mark J Millan, John D Pediani, Richard J Ward, Graeme Milligan
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a substantial proportion of the receptor was present within dimeric/oligomeric complexes and that increased expression levels of the receptor favored a greater dimer to monomer ratio. Addition of the antipsychotics, spiperone or haloperidol, resulted in re-organization of D3R quaternary structure to promote monomerization...
May 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28522842/cryo-electron-microscopy-structure-of-the-macrobrachium-rosenbergii-nodavirus-capsid-at-7-angstroms-resolution
#20
Kok Lian Ho, Chare Li Kueh, Poay Ling Beh, Wen Siang Tan, David Bhella
White tail disease in the giant freshwater prawn Macrobrachium rosenbergii causes significant economic losses in shrimp farms and hatcheries and poses a threat to food-security in many developing countries. Outbreaks of Macrobrachium rosenbergii nodavirus (MrNV), the causative agent of white tail disease (WTD) are associated with up to 100% mortality rates. There are no interventions available to treat or prevent MrNV disease however. Here we show the structure of MrNV virus-like particles (VLPs) produced by recombinant expression of the capsid protein, using cryogenic electron microscopy...
May 18, 2017: Scientific Reports
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