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https://www.readbyqxmd.com/read/28822281/an-integrative-study-to-identify-novel-scaffolds-for-sphingosine-kinase-1-inhibitors
#1
Marcela Vettorazzi, Emilio Angelina, Santiago Lima, Tomas Gonec, Jan Otevrel, Pavlina Marvanova, Tereza Padrtova, Petr Mokry, Pavel Bobal, Lina M Acosta, Alirio Palma, Justo Cobo, Janette Bobalova, Jozef Csollei, Ivan Malik, Sergio Alvarez, Sarah Spiegel, Josef Jampilek, Ricardo D Enriz
Sphingosine kinase 1 (SphK1), the enzyme that produces the bioactive sphingolipid metabolite, sphingosine-1-phosphate, is a promising new molecular target for therapeutic intervention in cancer and inflammatory diseases. In view of its importance, the main objective of this work was to find new and more potent inhibitors for this enzyme possessing different structural scaffolds than those of the known inhibitors. Our theoretical and experimental study has allowed us to identify two new structural scaffolds (three new compounds), which could be used as starting structures for the design and then the development of new inhibitors of SphK1...
August 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28822248/tio2-nanoparticles-in-sediments-effect-on-the-bioavailability-of-heavy-metals-in-the-freshwater-bivalve-corbicula-fluminea
#2
Xiulei Fan, Chao Wang, Peifang Wang, Bin Hu, Xun Wang
Most studies investigating the influence of TiO2 NPs on heavy metal bioavailability have focused on the aqueous phase; however, few have examined the sediments containing more nanoparticles. Here, we investigated the effects of TiO2 NPs on heavy metal bioavailability in C. fluminea in sediments. The interactions between the TiO2 NPs and metals in sediments, the influence of TiO2 NPs on metals levels in aqueous phase and geochemical speciation were also explored. The results indicated the large adsorption capacity of TiO2 NPs and the strong adsorption affinity to metals caused the metals adsorbed on nanoparticles, which decreased the metals concentrations in water phase...
July 21, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28822091/effect-of-ap102-a-subtype-2-and-5-specific-somatostatin-analog-on-glucose-metabolism-in-rats
#3
Erika Tarasco, Petra Seebeck, Svende Pfundstein, Adrian F Daly, Philippe J Eugster, Alan G Harris, Eric Grouzmann, Thomas A Lutz, Christina N Boyle
PURPOSE: Somatostatin analogs are widely used to treat conditions associated with hormonal hypersecretion such as acromegaly and metastatic neuroendocrine tumors. First generation somatostatin analogs, such as octreotide and lanreotide, have high affinity for somatostatin receptor subtype 2 (SSTR2), but have incomplete efficacy in many patients. Pasireotide targets multiple SSTRs, having the highest affinity for SSTR5, but causes hyperglycemia and diabetes mellitus in preclinical and clinical studies...
August 18, 2017: Endocrine
https://www.readbyqxmd.com/read/28821669/transcriptomic-analysis-of-ribosome-bound-mrna-in-cortical-neurites-in-vivo
#4
Rebecca Ouwenga, Allison M Lake, David O'Brien, Amit Mogha, Adish Dani, Joseph D Dougherty
Localized translation in neurites helps regulate synaptic strength and development. Dysregulation of local translation is associated with many neurological disorders. However, due to technical limitations, study of this phenomenon has largely been limited to brain regions with laminar organization of dendrites such as the hippocampus or cerebellum. It has not been examined in the cortex, a region of importance for most neurological disorders, where dendrites of each neuronal population are densely intermingled with cell bodies of others...
August 8, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28821665/molecular-and-functional-properties-of-regional-astrocytes-in-the-adult-brain
#5
Lydie Morel, Ming Sum R Chiang, Haruki Higashimori, Temitope Shoneye, Lakshmanan K Iyer, Julia Yelick, Albert Tai, Yongjie Yang
The molecular signature and functional properties of astroglial subtypes in the adult central nervous system (CNS) remain largely undefined. By employing translational ribosome affinity purification (TRAP) followed by RNA-seq, we profiled astroglial ribosome-associated (presumably translating) mRNAs in major cortical and subcortical brain regions (cortex, hippocampus, caudate putamen, nucleus accumbens, thalamus, and hypothalamus) of BAC aldh1l1-TRAP mice (both sexes). We found that the expression of astroglial translating mRNAs closely follows the dorsoventral axis especially from cortex/hippocampus to thalamus/hypothalamus posteriorly...
August 7, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28821619/dsc-e3-ligase-localization-to-the-golgi-requires-the-atpase-cdc48-and-cofactor-ufd1-for-activation-of-sterol-regulatory-element-binding-protein-in-fission-yeast
#6
Risa Burr, Diedre Ribbens, Sumana Raychaudhuri, Emerson V Stewart, Jason Ho, Peter J Espenshade
Sterol regulatory element-binding proteins (SREBPs) in the fission yeast Schizosaccharomyces pombe regulate lipid homeostasis and the hypoxic response under conditions of low sterol or oxygen availability. SREBPs are cleaved in the Golgi through the combined action of the Dsc E3 ligase complex, the rhomboid protease Rbd2, and the essential ATPases Associated with diverse cellular Activities (AAA+) ATPase Cdc48. The soluble SREBP N-terminal transcription factor domain is then released in the cytosol to enter the nucleus and regulate gene expression...
August 18, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28821615/distinct-structural-mechanisms-determine-substrate-affinity-and-kinase-activity-of-protein-kinase-c%C3%AE
#7
Sangbae Lee, Titu Devamani, Hyun Deok Song, Manbir Sandhu, Adrien Larsen, Ruth Sommese, Abhinandan Jain, Nagarajan Vaidehi, Sivaraj Sivaramakrishnan
Protein kinase Cα (PKCα) belongs to the family of AGC kinases that phosphorylate multiple peptide substrates. While the consensus sequence motif has been identified and used to explain substrate specificity for PKCα, it does not inform the structural basis of substrate binding and kinase activity for diverse substrates phosphorylated by this kinase. The transient, dynamic, and unstructured nature of this protein-protein interaction has limited structural mapping of kinase-substrate interfaces. Here, using multiscale MD simulation-based predictions and FRET sensor-based experiments, we investigated the conformational dynamics of the kinase-substrate interface...
August 15, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28821613/the-rir-motif-in-the-scaffold-protein-xrcc1-mediates-a-low-affinity-interaction-with-polynucleotide-kinase-phosphatase-pnkp-during-dna-single-strand-break-repair
#8
Claire Breslin, Rajam S Mani, Mesfin Fanta, Nicolas Hoch, Michael Weinfeld, Keith W Caldecott
The scaffold protein X-ray repair cross-complementing 1 (XRCC1) interacts with multiple enzymes involved in DNA base excision repair and single-strand break repair (SSBR) and is important for genetic integrity and normal neurological function. One of the most important interactions of XRCC1 is that with polynucleotide kinase/phosphatase (PNKP), a dual-function DNA kinase/phosphatase that processes damaged DNA termini and that, if mutated, results in ataxia with oculomotor apraxia 4 (AOA4) and microcephaly with early-onset seizures and developmental delay (MCSZ)...
August 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28821611/the-proteasome-interacting-ecm29-protein-disassembles-the-26s-proteasome-in-response-to-oxidative-stress
#9
Xiaorong Wang, Ilan E Chemmama, Clinton Yu, Alexander Huszagh, Yue Xu, Rosa Viner, Sarah Ashley Block, Peter Cimermancic, Scott D Rychnovsky, Yihong Ye, Andrej Sali, Lan Huang
Oxidative stress has been implicated in multiple human neurological and other disorders. Proteasomes are multi-subunit proteases critical for the removal of oxidatively damaged proteins. To understand stress-associated human pathologies, it is important to uncover the molecular events underlying the regulation of proteasomes upon oxidative stress. To this end, we investigated H2O2 stress-induced molecular changes of the human 26S proteasome and determined that stress-induced 26S proteasome disassembly is conserved from yeast to human...
August 15, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28821604/development-of-a-multiplexed-assay-for-oral-cancer-candidate-biomarkers-using-peptide-immunoaffinity-enrichment-and-targeted-mass-spectrometry
#10
Yung-Chin Hsiao, Lang-Ming Chi, Kun-Yi Chien, Wei-Fan Chiang, Szu-Fan Chen, Yao-Ning Chuang, Shih-Yu Lin, Chia-Chun Wu, Ya-Ting Chang, Lichieh Julie Chu, Yi-Ting Chen, Shu-Li Chia, Chih-Yen Chien, Kai-Ping Chang, Yu-Sun Chang, Jau-Song Yu
Oral cancer is one of the most common cancers worldwide, and there are currently no biomarkers approved for aiding its management. Although many potential oral cancer biomarkers have been discovered, very few have been verified in body fluid specimens in parallel to evaluate their clinical utility. The lack of appropriate multiplexed assays for chosen targets represents one of the bottlenecks to achieving this goal. In the present study, we develop a peptide immunoaffinity enrichment-coupled multiple reaction monitoring-mass spectrometry (SISCAPA-MRM) assay for verifying multiple reported oral cancer biomarkers in saliva...
August 18, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28821545/heterologous-production-of-thermophile-thermochromatium-tepidum-photosynthetic-reaction-centre-and-light-harvesting-1-complexes-in-the-mesophile-rhodobacter-sphaeroides-and-thermal-stabilities-of-a-hybrid-core-complex
#11
D Jun, V Huang, J T Beatty
The photosynthetic complexes of the thermophile Thermochromatium tepidum are of considerable interest in biohybrid solar cell applications because of the capability of thermophilic proteins to tolerate elevated temperatures. Synthetic operons encoding reaction centre (RC) and light harvesting 1 (LH1) pigment-protein complexes of T. tepidum were expressed in the mesophile Rhodobacter sphaeroides The T. tepidum RC (TRC) was assembled, and functional with the addition of menadione to populate the QA pocket. The production of the T...
August 18, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28821542/human-hepatocyte-metabolism-of-novel-synthetic-cannabinoids-mn-18-and-its-5-fluoro-analog-5f-mn-18
#12
Xingxing Diao, Jeremy Carlier, Mingshe Zhu, Marilyn A Huestis
BACKGROUND: In 2014, 2 novel synthetic cannabinoids, MN-18 and its 5-fluoro analog, 5F-MN-18, were first identified in an ongoing survey of novel psychoactive substances in Japan. In vitro pharmacological assays revealed that MN-18 and 5F-MN-18 displayed high binding affinities to human CB1 and CB2 receptors, with Ki being 1.65-3.86 nmol/L. MN-18 and 5F-MN-18 were scheduled in Japan and some other countries in 2014. Despite increasing prevalence, no human metabolism data are currently available, making it challenging for forensic laboratories to confirm intake of MN-18 or 5F-MN-18...
August 18, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28821092/the-effect-of-temperature-on-the-colligative-properties-of-food-grade-konjac-gum-in-water-solutions
#13
Joanna Kruk, Kacper Kaczmarczyk, Anna Ptaszek, Urszula Goik, Paweł Ptaszek
This research paper presents the results of tests on the colligative properties of konjac gum chains in water solutions. For this purpose, the measurements of osmotic pressure and intrinsic viscosity of aqueous solutions, in the function of konjac gum concentration and temperature were carried out. The applied methods allowed for the determination of the second osmotic virial coefficients B2, which raised with the increase of temperature. It indicate that increase of temperature causes higher affinity of polysaccharide's chains to water...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28821072/understanding-the-mechanisms-of-oxygen-diffusion-through-surface-functionalized-nanocellulose-films
#14
Maria Soledad Peresin, Kari Kammiovirta, Harri Heikkinen, Leena-Sisko Johansson, Jari Vartiainen, Harri Setälä, Monika Österberg, Tekla Tammelin
A concept for direct surface modification on self-standing films of cellulose nanofibrils (CNF) is demonstrated using an aminosilane group in cellulose compatible solvent (dimethyl acetamide, DMA). The chemically modified structure efficiently prevents the oxygen molecules from interacting with the nanocellulose film in the presence of water molecules. Oxygen permeability values lower than 1mLmmm(-2)day(-1)atm(-1) were achieved at extremely high levels of relative humidity (RH95%). The aminosilane reaction is compared to conventional hydrophobization reaction using hexamethyldisilazane...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28821061/morphology-and-mechanical-properties-of-poly-%C3%AE-hydroxybutyrate-poly-%C3%AE%C2%B5-caprolactone-blends-controlled-with-cellulosic-particles
#15
Jianxiang Chen, Yuankun Wang, Zeren Yin, Kam C Tam, Defeng Wu
The rigid microcrystalline cellulose (MCC) particles and semi-rigid ethyl cellulose (EC) were used to control phase morphology and mechanical properties of immiscible poly(β-hydroxybutyrate) (PHB)/poly(ε-caprolactone) (PCL) blends. The interfacial properties were evaluated by the fiber retraction and contact angle methods MCC is incompatible with PHB and PCL, and dispersed independently in the two polymer phases in their blends. However, EC is more compatible with the two polymers, with a higher affinity for PCL...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28821003/-111-in-dtpa-d-phe-1-asp-0-d-phe-1-octreotide-exhibits-higher-tumor-accumulation-and-lower-renal-radioactivity-than-111-in-dtpa-d-phe-1-octreotide
#16
Nobuhiro Oshima, Hiromichi Akizawa, Hirotake Kitaura, Hidekazu Kawashima, Songji Zhao, Yan Zhao, Ken-Ichi Nishijima, Yoji Kitamura, Yasushi Arano, Yuji Kuge, Kazue Ohkura
INTRODUCTION: (111)In-DTPA-d-Phe(1)-octreotide scintigraphy is an important method of detecting neuroendocrine tumors. We previously reported that a new derivative of (111)In-DTPA-d-Phe(1)-octreotide, (111)In-DTPA-d-Phe(-1)-Asp(0)-d-Phe(1)-octreotide, accomplished the reduction of prolonged renal accumulation of radioactivity. The aim of this study was to evaluate the tumor accumulation of (111)In-DTPA-d-Phe(-1)-Asp(0)-d-Phe(1)-octreotide in vitro and in vivo by comparing it with (111)In-DTPA-d-Phe(1)-octreotide...
July 12, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28820984/identification-of-m-tuberculosis-antigens-in-the-sera-of-tuberculosis-patients-using-biomimetic-affinity-chromatography-in-conjunction-with-esi-cid-ms-ms
#17
Guorong Ma, Jinting Pan, Jincheng Han, Lina Gao, Shulin Zhang, Rongxiu Li
The profiling of abnormally-expressed proteins in host cells using mass spectrometry (MS) analysis is a classical approach for screening disease-associated biomarkers in clinical diagnosis. However, few pathogen-specific antigens can currently be detected in serum using this proteomic approach, since these are very low-abundant proteins that are easily masked by host high-abundant proteins. Identification of pathogen-specific antigens in the sera of tuberculosis patients is crucial for the clinical diagnosis of this infectious disease, especially in immune-compromised patients...
July 31, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28820982/direct-analysis-no-sample-preparation-of-bioavailable-cortisol-in-human-plasma-by-weak-affinity-chromatography-wac
#18
Sten Ohlson, Jagjit Kaur, Manfred Raida, Ulf Niss, Tim Bengala, Chester Lee Drum, Bernhard Boehm, Anthony R Torres
Pre-analytical treatment of blood plasma is a time consuming and often rate limiting step in the workflow of LC/MS analysis. We present in this pilot study a new approach for quantitative LC/MS based on weak affinity chromatography (WAC) of crude plasma. The steroid hormone cortisol was selected as a clinically relevant biomarker, as it currently requires extensive pre-analytical preparation. A WAC unit with saturating, immobilized albumin as a prototypic weak binder was used in combination with an ion-funnel MS/MS detector to perform zonal affinity chromatography of cortisol directly from a plasma sample, followed by quantitative multiple reaction monitoring (MRM)...
July 21, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28820969/a-disulfide-stabilized-human-vl-single-domain-antibody-library-is-a-source-of-soluble-and-highly-thermostable-binders
#19
Kevin A Henry, Hiba Kandalaft, Michael J Lowden, Martin A Rossotti, Henk van Faassen, Greg Hussack, Yves Durocher, Dae Young Kim, Jamshid Tanha
We have previously shown that incorporation of a second intradomain disulfide linkage into camelid VHH and human VH/VL single-domain antibodies confers increased thermostability. Here, we explored the effects of introducing an additional disulfide linkage, formed between Cys48 and Cys64 (Kabat numbering), into a phage-displayed synthetic human VL library. In comparison to an identical library bearing only the highly conserved Cys23-Cys88 disulfide linkage, the disulfide-stabilized VL library tolerated a similar degree of randomization but retained a higher level of functional diversity after selection with protein L...
August 15, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28820936/elucidating-substrate-promiscuity-within-the-fabi-enzyme-family
#20
Gabriel S Freund, Terrence E O'Brien, Logan Vinson, Dylan Alexander Carlin, Andrew Yao, Wai Shun Mak, Ilias Tagkopoulos, Marc T Facciotti, Dean J Tantillo, Justin B Siegel
The rapidly growing appreciation of enzymes' catalytic and substrate promiscuity may lead to their expanded use in the fields of chemical synthesis and industrial biotechnology. Here we explore the substrate promiscuity of enoyl-acyl carrier protein reductases (commonly known as FabI), and how that promiscuity is a function of inherent reactivity and the geometric demands of the enzyme's active site. We demonstrate that these enzymes catalyze the reduction of a wide range of substrates, particularly α,β-unsaturated aldehydes...
August 18, 2017: ACS Chemical Biology
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