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https://www.readbyqxmd.com/read/27914362/an-overview-of-the-binding-models-of-fgfr-tyrosine-kinases-in-complex-with-small-molecule-inhibitors
#1
REVIEW
Weiyan Cheng, Mixiang Wang, Xin Tian, Xiaojian Zhang
The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3, and FGFR4. Given its intimate role in the progression of several solid tumors, excessive FGFR signaling provides an opportunity for anticancer therapy. Along with extensive pharmacological studies validating the therapeutic potential of targeting the FGFRs for cancer treatment, co-crystal structures of FGFRs/inhibitors are continuously coming up to study the mechanism of actions and explore new inhibitors...
November 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914132/associations-between-soluble-receptor-for-advanced-glycation-end-products-srage-and-s100a12-en-rage-with-mortality-in-long-term-hemodialysis-patients
#2
Eul Sik Jung, Wookyung Chung, Ae Jin Kim, Han Ro, Jae Hyun Chang, Hyun Hee Lee, Ji Yong Jung
Hemodialysis (HD) patients experience vascular calcification, ultimately leading to high mortality rates. Previously, we reported associations between soluble receptor for advanced glycation end products (sRAGEs) and extracellular newly identified RAGE-binding protein S100A12 (EN-RAGE) and vascular calcification. Here, we extended our observations, investigating whether these biomarkers may be useful for predicting cardiovascular morbidity and mortality in these subjects. Thus, we evaluated the relationship between sRAGE and S100A12 and mortality in long-term HD patients...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914066/computational-tools-for-allosteric-drug-discovery-site-identification-and-focus-library-design
#3
Wenkang Huang, Ruth Nussinov, Jian Zhang
Allostery is an intrinsic phenomenon of biological macromolecules involving regulation and/or signal transduction induced by a ligand binding to an allosteric site distinct from a molecule's active site. Allosteric drugs are currently receiving increased attention in drug discovery because drugs that target allosteric sites can provide important advantages over the corresponding orthosteric drugs including specific subtype selectivity within receptor families. Consequently, targeting allosteric sites, instead of orthosteric sites, can reduce drug-related side effects and toxicity...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27914014/experimental-and-theoretical-investigation-of-sodiated-multimers-of-steroid-epimers-with-ion-mobility-mass-spectrometry
#4
Christopher D Chouinard, Vinícius Wilian D Cruzeiro, Adrian E Roitberg, Richard A Yost
Ion mobility-mass spectrometry (IM-MS) has recently seen increased use in the analysis of small molecules, especially in the field of metabolomics, for increased breadth of information and improved separation of isomers. In this study, steroid epimers androsterone and trans-androsterone were analyzed with IM-MS to investigate differences in their relative mobilities. Although sodiated monomers exhibited very similar collision cross-sections (CCS), baseline separation was observed for the sodiated dimer species (RS = 1...
December 2, 2016: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/27913923/actn3-x-allele-carriers-had-greater-levels-of-muscle-damage-during-a-half-ironman
#5
Juan Del Coso, Juan José Salinero, Beatriz Lara, César Gallo-Salazar, Francisco Areces, Carlos Puente, David Herrero
PURPOSE: Alpha-actinin-3, encoded by the ACTN3 gene, is an actin-binding protein with an important role in myofibril contraction and muscle force output. In humans, there is a relatively common deficiency of the α-actinin-3 due to homozygosity in a polymorphism of the ACTN3 gene (R577X, rs1815739), that has been related to decreased resistance to strain during voluntary muscle contractions. The purpose of this study was to investigate the influence of the ACTN3 genotype on the level of exercise-induced muscle damage attained by 23 experienced triathletes during an official half-ironman competition...
December 2, 2016: European Journal of Applied Physiology
https://www.readbyqxmd.com/read/27913823/mathematical-models-suggest-facilitated-fatty-acids-crossing-of-the-luminal-membrane-in-the-cardiac-muscle
#6
Efrath Barta
Long-chain fatty acids cross a few membranes on their way from the capillary blood to the cardiomyocyte cytosol, where they are utilized as an essential source of energy. Details of the transport mechanism across those membranes remained elusive despite decades of laboratory and theoretical work. Here we inspect several optional scenarios for the crossing of the luminal membrane of the endothelial cell, the first barrier that should be crossed: a passive diffusion, facilitation by receptors for albumin and facilitation by fatty acids transporters...
December 3, 2016: Journal of Membrane Biology
https://www.readbyqxmd.com/read/27913817/the-contribution-of-response-conflict-multisensory-integration-and-body-mediated-attention-to-the-crossmodal-congruency-effect
#7
Francesco Marini, Daniele Romano, Angelo Maravita
The crossmodal congruency task is a consolidated paradigm for investigating interactions between vision and touch. In this task, participants judge the elevation of a tactile target stimulus while ignoring a visual distracter stimulus that may occur at a congruent or incongruent elevation, thus engendering a measure of visuo-tactile interference (crossmodal congruency effect, CCE). The CCE reflects perceptual, attentional, and response-related factors, but their respective roles and interactions have not been set out yet...
December 2, 2016: Experimental Brain Research. Experimentelle Hirnforschung. Expérimentation Cérébrale
https://www.readbyqxmd.com/read/27913665/structure-and-function-of-bacterial-h-ns-protein
#8
REVIEW
David C Grainger
The histone-like nucleoid structuring (H-NS) protein is a major component of the folded chromosome in Escherichia coli and related bacteria. Functions attributed to H-NS include management of genome evolution, DNA condensation, and transcription. The wide-ranging influence of H-NS is remarkable given the simplicity of the protein, a small peptide, possessing rudimentary determinants for self-association, hetero-oligomerisation and DNA binding. In this review, I will discuss our understanding of H-NS with a focus on these structural elements...
December 15, 2016: Biochemical Society Transactions
https://www.readbyqxmd.com/read/27913641/translation-repression-by-maternal-rna-binding-protein-zar1-is-essential-for-early-oogenesis-in-zebrafish
#9
Liyun Miao, Yue Yuan, Feng Cheng, Junshun Fang, Fang Zhou, Weirui Ma, Yan Jiang, Xiahe Huang, Yingchun Wang, Lingjuan Shan, Dahua Chen, Jian Zhang
Large numbers of maternal RNAs are deposited in oocytes and are reserved for later development. Control of maternal RNA translation during oocyte maturation has been extensively investigated and its regulatory mechanisms are well documented. However, translational regulation of maternal RNAs in early oogenesis is largely unexplored. In this study, we generated zebrafish zar1 mutants which result in early oocyte apoptosis and fully penetrant male development. Loss of p53 suppresses the apoptosis in zar1 mutants and restores oocyte development...
December 2, 2016: Development
https://www.readbyqxmd.com/read/27913634/comparative-analysis-highlights-variable-genome-content-of-wheat-rusts-and-divergence-of-the-mating-loci
#10
Christina A Cuomo, Guus Bakkeren, Hala Badr Khalil, Vinay Panwar, David Joly, Rob Linning, Sharadha Sakthikumar, Xiao Song, Xian Adiconis, Lin Fan, Jonathan M Goldberg, Joshua Z Levin, Sarah Young, Qiandong Zeng, Yehoshua Anikster, Myron Bruce, Meinan Wang, Chuntao Yin, Brent McCallum, Les J Szabo, Scot Hulbert, Xiaming Chen, John P Fellers
Three members of the Puccinia genus, P. triticina (Pt), P. striiformis f.sp. tritici (Pst), and P. graminis f.sp. tritici (Pgt), cause the most common and often most significant foliar diseases of wheat. While similar in biology and life cycle, each species is uniquely adapted and specialized. The genomes of Pt and Pst were sequenced and compared to that of Pgt to identify common and distinguishing gene content, to determine gene variation among wheat rust pathogens, other rust fungi and basidiomycetes, and to identify genes of significance for infection...
December 2, 2016: G3: Genes—Genomes—Genetics
https://www.readbyqxmd.com/read/27913545/what-have-we-learned-from-large-population-studies-of-von-willebrand-disease
#11
Robert R Montgomery, Veronica H Flood
Von Willebrand factor (VWF) is a critical regulator of hemostatic processes, including collagen binding, platelet adhesion, and platelet aggregation. It also serves as a carrier protein to normalize plasma factor VIII synthesis, release, and survival. While VWF protein measurements by immunoassay are reasonably comparable between institutions, the measurement of VWF ristocetin cofactor activity (VWF:RCo) has significant variability. Other tests of VWF function, including collagen binding or platelet glycoprotein IIb-IIIa binding, are not universally available, yet these functional defects may cause major bleeding even with normal VWF antigen (VWF:Ag) and VWF:RCo assays...
December 2, 2016: Hematology—the Education Program of the American Society of Hematology
https://www.readbyqxmd.com/read/27913295/dissection-of-functional-lncrnas-in-alzheimer-s-disease-by-construction-and-analysis-of-lncrna-mrna-networks-based-on-competitive-endogenous-rnas
#12
Lian-Kun Wang, Xiao-Feng Chen, Dan-Dan He, You Li, Jin Fu
Alzheimer's disease (AD) is a neurodegenerative disorder that is the most common cause of dementia in the elderly, and intracellular neurofibrillary tangles (NFTs) are one of the pathological features of AD. Recent studies have suggested long noncoding RNAs (lncRNAs) play important roles in AD. Competing endogenous RNAs (ceRNAs) is a mechanism that has recently been proposed, in which lncRNAs compete for common miRNA-binding sites with mRNAs. However, the roles of lncRNAs and ceRNA in AD NFTs is limited. In this study, we constructed a global triple network based on ceRNA theory, then an AD NFT lncRNA-mRNA network (NFTLMN) was generated...
November 29, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27913257/prodynorphin-and-kappa-opioid-receptor-mrna-expression-in-the-brain-relates-to-social-status-and-behavior-in-male-european-starlings
#13
Lauren V Riters, Melissa A Cordes, Sharon A Stevenson
Numerous animal species display behavioral changes in response to changes in social status or territory possession. For example, in male European starlings only males that acquire nesting sites display high rates of sexual and agonistic behavior. Past studies show that mu and delta opioid receptors regulate behaviors associated with social ascension or defeat. Opioids also act at kappa receptors, with dynorphin binding with the highest affinity; however, the role of these opioids in social behavior has not been well studied...
November 29, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27913103/ontogeny-aging-and-gender-related-changes-in-hepatic-multidrug-resistant-protein-genes-in-rats
#14
Qiong-Ni Zhu, Wei-Yu Hou, Shang-Fu Xu, Yuan-Fu Lu, Jie Liu
: Multidrug resistance proteins (Mrps) are efflux transporters playing important roles in endogenous substances and xenobiotics transport out of the liver. Children, elderly, gender and physio-pathological conditions could influence their expression and result in changes in drug disposition. AIM: This study was aimed to examine the development-, ageing-, and sex-dependent changes in Mrp1-4 and ATP-binding cassette sub-family G member 2 (Abcg2) gene expressions in livers of rats...
November 29, 2016: Life Sciences
https://www.readbyqxmd.com/read/27913018/potential-impact-of-flowback-water-from-hydraulic-fracturing-on-agricultural-soil-quality-metal-metalloid-bioaccessibility-microtox-bioassay-and-enzyme-activities
#15
Season S Chen, Yuqing Sun, Daniel C W Tsang, Nigel J D Graham, Yong Sik Ok, Yujie Feng, Xiang-Dong Li
Hydraulic fracturing has advanced the development of shale gas extraction, while inadvertent spills of flowback water may pose a risk to the surrounding environment due to its high salt content, metals/metalloids (As, Se, Fe and Sr), and organic additives. This study investigated the potential impact of flowback water on four representative soils from shale gas regions in Northeast China using synthetic flowback solutions. The compositions of the solutions were representative of flowback water arising at different stages after fracturing well establishment...
November 29, 2016: Science of the Total Environment
https://www.readbyqxmd.com/read/27912771/a-dna-vaccine-encoding-the-viral-hemorrhagic-septicemia-virus-genotype-ivb-glycoprotein-confers-protection-in-muskellunge-esox-masquinongy-rainbow-trout-oncorhynchus-mykiss-brown-trout-salmo-trutta-and-lake-trout-salvelinus-namaycush
#16
Isaac F Standish, Elena V Millard, Travis O Brenden, Mohamed Faisal
BACKGROUND: The viral hemorrhagic septicemia virus (VHSV) is one of the most serious fish pathogens. In 2003, a novel sublineage (genotype IVb) of this deadly virus emerged in the Great Lakes basin causing serious fish kills. We have previously demonstrated that a DNA plasmid (pcDNA), containing a cytomegalovirus (CMV) promoter and the viral hemorrhagic septicemia virus (VHSV) genotype IVb glycoprotein (G) gene insert (designated pVHSivb-G) confers moderate protection in muskellunge (Esox masquinongy), a highly susceptible species upon challenge...
December 2, 2016: Virology Journal
https://www.readbyqxmd.com/read/27912738/hepatoprotective-activity-of-lepidium-sativum-seeds-against-d-galactosamine-lipopolysaccharide-induced-hepatotoxicity-in-animal-model
#17
Mohammad Raish, Ajaz Ahmad, Khalid M Alkharfy, Syed Rizwan Ahamad, Kazi Mohsin, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea, Mushtaq Ahmad Ansari
BACKGROUND: Fulminant hepatic failure (FHF) is clinical syndrome with very poor prognosis and high mortality there is urgent need for the development of safe and non-toxic hepatoprotective agents for the adequate management of hepatitis. Hepatoprotective effect of the Lepidium sativum ethanolic extract (LSEE) was assessed by D-galactosamine-induced/lipopolysaccharide (400 mg/kg and 30 μg/kg) liver damage model in rats. METHODS: Hepatoprotective activity of LSEE (150 and 300 mg/kg) and silymarin on D-GalN/LPS induced FHF in rat was assessed using several liver function enzyme parameters...
December 3, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27912177/raman-spectroscopy-and-quantum-mechanical-analysis-of-tautomeric-forms-in-cytosine-and-5-methylcytosine-on-gold-surfaces
#18
Dinh Bao Nguyen, Thanh Danh Nguyen, Sangsoo Kim, Sang-Woo Joo
Spectral differences between cytosine (Cyt) and 5-methylcytosine (5MC) were investigated by means of Raman spectroscopy with a combination of density functional theory (DFT) calculations. Surface-enhanced Raman scattering (SERS) revealed discriminating peaks of 5MC from those of Cyt upon adsorption on gold nanoparticles (AuNPs). Among the notable features, the multiple bands between 850 and 700cm(-1) for the ring-breathing modes of 5MC and Cyt could be correlated well with the simulated spectra based on the DFT calculations of the adsorbates on the gold cluster atoms...
November 9, 2016: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/27912076/activating-transcription-factor-3-is-essential-for-cigarette-smoke-induced-mucin-expression-via-interaction-with-activator-protein-1
#19
Yan-Ping Wu, Yin-Fang Wu, Chao Zhang, Hong-Bin Zhou, Chao Cao, Miao Li, Chen Zhu, Song-Min Ying, Zhi-Hua Chen, Hua-Hao Shen, Wen Li
Mucus hypersecretion is an important pathologic feature of chronic obstructive pulmonary disease. Activating transcription factor 3 (ATF3) is an adaptive-response gene that participates in various cellular processes. However, little is known about its role in cigarette smoke (CS)-induced mucus hyperproduction. This study aimed to investigate the role and molecular mechanisms of ATF3 in CS-induced Mucin 5AC (MUC5AC) expression. ATF3 was elevated in lung tissues of mice exposed to CS for 12 weeks. Treatment with CS extract significantly induced ATF3 expression and MUC5AC production in human bronchial epithelial cells, NCI-H292, and mouse tracheal epithelial cells...
November 29, 2016: American Journal of Pathology
https://www.readbyqxmd.com/read/27911878/y-box-binding-protein-1-promotes-hepatocellular-carcinomainitiating-cell-progression-and-tumorigenesis-via-wnt-%C3%AE-catenin-pathway
#20
Hsiao-Mei Chao, Hong-Xuan Huang, Po-Hsiang Chang, Kuo-Chang Tseng, Atsushi Miyajima, Edward Chern
Y-box binding protein-1 (YB-1) is a pleiotropic molecule that binds DNA to regulate genes on a transcriptional level in the nucleus and binds RNA to modulate gene translation in the cytoplasm. In our previous studies, YB-1 was also characterized as a fetal hepatic protein that regulates the maturation of hepatocytes and is upregulated during liver regeneration. Moreover, YB-1 has been shown to be expressed in human hepatocellular carcinoma (HCC). However, the role of YB-1 in HCC remains unclear. Here, we aimed to characterize the role of YB-1 in HCC...
December 1, 2016: Oncotarget
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