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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/27914341/single-crystalline-titanium-dioxide-hollow-tetragonal-nanocones-with-large-exposed-101-facets-for-excellent-photocatalysis
#2
Zhengcui Wu, Yejing Xue, Zexian Zou, Xia Wang, Feng Gao
Crystal facet engineering and surface modification of semiconductor have become important strategies to improve photocatalytic activity by optimizing surface charge carrier separation/transfer and extending solar spectrum utilization. In this work, we report anatase single-crystalline TiO2 hollow tetragonal nanocones with large exposed (101) facets by a facile liquid-phase interfacial synthetic strategy, using the hydrolysis of tetrabutyltitanate with adscititious water in the organic solvent of cyclohexane and a capping agent of 1, 6-hexanediamine...
November 23, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914300/structure-based-analysis-of-bacilli-and-plasmid-dihydrofolate-reductase-evolution
#3
Mona Alotaibi, Ben Delos Reyes, Tin Le, Phuong Luong, Faramarz Valafar, Robert P Metzger, Gary B Fogel, David Hecht
Dihydrofolate reductase (DHFR), a key enzyme in tetrahydrofolate-mediated biosynthetic pathways, has a structural motif known to be highly conserved over a wide range of organisms. Given its critical role in purine and amino acid synthesis, DHFR is a well established therapeutic target for treating a wide range of prokaryotic and eukaryotic infections as well as certain types of cancer. Here we present a structural-based computer analysis of bacterial (Bacilli) and plasmid DHFR evolution. We generated a structure-based sequence alignment using 7 wild-type DHFR x-ray crystal structures obtained from the RCSB Protein Data Bank and 350 chromosomal and plasmid homology models we generated from sequences obtained from the NCBI Protein Database...
November 22, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27914179/ammonothermal-synthesis-of-novel-nitrides-case-study-on-cagasin3
#4
Jonas Häusler, Lukas Neudert, Mathias Mallmann, Robin Niklaus, Anna-Carina L Kimmel, Nicolas S A Alt, Eberhard Schlücker, Oliver Oeckler, Wolfgang Schnick
The first gallium-containing nitridosilicate CaGaSiN3 was synthesized in newly developed high-pressure autoclaves using supercritical ammonia as solvent and nitriding agent. The reaction was conducted in ammonobasic environment starting from intermetallic CaGaSi with NaN3 as mineralizer. At 770 K, intermediate compounds were obtained, which were subsequently converted to the crystalline nitride at temperatures up to 1070 K (70 - 150 MPa). The impact of other mineralizers (e. g. LiN3, KN3 and CsN3) on the product formation was investigated as well...
December 3, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27914093/lsmo-nanoparticles-coated-by-hyaluronic-acid-for-magnetic-hyperthermia
#5
Yuanwei Chen, Ying Wang, Xi Liu, Mai Lu, Jiangwei Cao, Tao Wang
Magnetic hyperthermia with the treating temperature range of 41-46 °C is an alternative therapy for cancer treatment. In this article, lanthanum strontium manganates (La1-x Sr x MnO3, 0.25 ≤ × ≤ 0.35) magnetic nanoparticles coated by hyaluronic acid (HA) which possesses the ability of targeting tumor cells were prepared by a simple hydrothermal method combined with a high-energy ball milling technique. The crystal structure, morphology, magnetic properties of the HA-coated magnetic nanoparticles (MNPs), and their heating ability under alternating magnetic field were investigated...
December 2016: Nanoscale Research Letters
https://www.readbyqxmd.com/read/27914074/common-challenges-in-studying-the-structure-and-function-of-bacterial-proteins-case-studies-from-helicobacter-pylori
#6
Daniel A Bonsor, Eric J Sundberg
Employing biophysical and structural methods is a powerful way to elucidate mechanisms of molecular recognition in bacterial pathogenesis. Such studies invariably depend on the production of pure, folded and stable proteins. Many proteins that can be expressed recombinantly ultimately fail to meet one or more of these criteria. The cag proteins from Helicobacter pylori form a secretion system that delivers the oncoprotein, CagA, into human gastric epithelial cells through an interaction between CagL and host cell integrins, where it can cause gastric adenocarcinoma...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27913993/antifreeze-glycopeptides-from-structure-and-activity-studies-to-current-approaches-in-chemical-synthesis
#7
REVIEW
Małgorzata Urbańczyk, Jerzy Góra, Rafał Latajka, Norbert Sewald
Antifreeze glycopeptides (AFGPs) are a class of biological antifreeze agents found predominantly in Arctic and Antarctic species of fish. They possess the ability to regulate ice nucleation and ice crystal growth, thus creating viable life conditions at temperatures below the freezing point of body fluids. AFGPs usually consist of 4-55 repetitions of the tripeptide unit Ala-Ala-Thr that is O-glycosylated at the threonine side chains with β-D-galactosyl-(1 → 3)-α-N-acetyl-D-galactosamine. Due to their interesting properties and high antifreeze activity, they have many potential applications, e...
December 2, 2016: Amino Acids
https://www.readbyqxmd.com/read/27913850/two-novel-cyclic-hexapeptides-from-the-genetically-engineered-actinosynnema-pretiosum
#8
Chunhua Lu, Fei Xie, Chuan Shan, Yuemao Shen
Two novel cyclic hexapeptides designated actinosynneptides A (1) and B (2), together with three tryptophan containing diketopiperazines, namely cyclo(L-Trp-L-Trp) (3), cyclo(L-Trp-N-MeL-Trp) (4), and cyclo(N-MeL-Trp-N-MeL-Trp) (5), were isolated from the culture of the genetically engineered strain HGF052::asm18 derived from Actinosynnema pretiosum ATCC31565. Their structures were elucidated on the basis of spectroscopic analyses and single-crystal X-ray diffractions. Compound 1 is the first example of 3-amino-6-hydroxy-2-piperidone-containing cyclic peptides, and 1 and 2 showed moderate cytotoxic activities against HeLa and PC3 cell lines...
December 2, 2016: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/27913732/a-hydantoin-isoform-of-cyclic-n6-threonylcarbamoyladenosine-ct6a-is-present-in-trnas
#9
Michal Matuszewski, Jakub Wojciechowski, Kenjyo Miyauchi, Zofia Gdaniec, Wojciech M Wolf, Tsutomu Suzuki, Elzbieta Sochacka
N(6)-Threonylcarbamoyladenosine (t(6)A) and its derivatives are universally conserved modified nucleosides found at position 37, 3' adjacent to the anticodon in tRNAs responsible for ANN codons. These modifications have pleiotropic functions of tRNAs in decoding and protein synthesis. In certain species of bacteria, fungi, plants and protists, t(6)A is further modified to the cyclic t(6)A (ct(6)A) via dehydration catalyzed by TcdA. This additional modification is involved in efficient decoding of tRNA(Lys) Previous work indicated that the chemical structure of ct(6)A is a cyclic active ester with an oxazolone ring...
December 2, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27913730/dna-recognition-by-the-swai-restriction-endonuclease-involves-unusual-distortion-of-an-8-base-pair-a-t-rich-target
#10
Betty W Shen, Daniel F Heiter, Keith D Lunnen, Geoffrey G Wilson, Barry L Stoddard
R.SwaI, a Type IIP restriction endonuclease, recognizes a palindromic eight base pair (bp) symmetric sequence, 5'-ATTTAAAT-3', and cleaves that target at its center to generate blunt-ended DNA fragments. Here, we report three crystal structures of SwaI: unbound enzyme, a DNA-bound complex with calcium ions; and a DNA-bound, fully cleaved complex with magnesium ions. We compare these structures to two structurally similar 'PD-D/ExK' restriction endonucleases (EcoRV and HincII) that also generate blunt-ended products, and to a structurally distinct enzyme (the HNH endonuclease PacI) that also recognizes an 8-bp target site consisting solely of A:T base pairs...
December 1, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27913623/chac2-an-enzyme-for-slow-turnover-of-cytosolic-glutathione
#11
Amandeep Kaur, Ruchi Gautam, Ritika Srivastava, Avinash Chandel, Akhilesh Kumar, Subramanian Karthikeyan, Anand Kumar Bachhawat
Glutathione degradation plays an important role in glutathione and redox homeostasis and thus it is imperative to understand the enzymes and the mechanisms involved in glutathione degradation in detail. We describe here ChaC2, a member of the ChaC family of γ-glutamylcyclotransferases, as an enzyme that degrades glutathione in the cytosol of mammalian cells. ChaC2 is distinct from the previously described ChaC1, to which ChaC2 shows about 50% sequence identity. Human and mouse ChaC2 proteins, purified in vitro, show 10-20 fold lower catalytic efficiency than ChaC1, although they showed comparable Km values (Km of 3...
December 2, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27913427/intermittent-hypoxia-during-recovery-from-neonatal-hyperoxic-lung-injury-causes-long-term-impairment-of-alveolar-development-a-new-rat-model-of-bpd
#12
Anastasiya Mankouski, Crystal Kantores, Mathew J Wong, Julijana Ivanovska, Amish Jain, Eric J Benner, Stanley N Mason, A Keith Tanswell, Richard L Auten, Robert P Jankov
Bronchopulmonary dysplasia (BPD) is a chronic lung injury characterized by impaired alveologenesis that may persist into adulthood. Rat models of BPD using varying degrees of hyperoxia to produce injury either cause early mortality or spontaneously recover following removal of the inciting stimulus, thus limiting clinical relevance. We sought to refine an established rat model induced by exposure to 60% O2 from birth by following hyperoxia with intermittent hypoxia (IH). Rats exposed from birth to air or 60% O2 until day 14 were recovered in air with or without IH (FiO2 = 0...
December 2, 2016: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/27912844/heparanase-from-basic-research-to-therapeutic-applications-in-cancer-and-inflammation
#13
Israel Vlodavsky, Preeti Singh, Ilanit Boyango, Lilach Gutter-Kapon, Michael Elkin, Ralph D Sanderson, Neta Ilan
Heparanase, the sole heparan sulfate degrading endoglycosidase, regulates multiple biological activities that enhance tumor growth, angiogenesis and metastasis. Heparanase expression is enhanced in almost all cancers examined including various carcinomas, sarcomas and hematological malignancies. Numerous clinical association studies have consistently demonstrated that upregulation of heparanase expression correlates with increased tumor size, tumor angiogenesis, enhanced metastasis and poor prognosis. In contrast, knockdown of heparanase or treatments of tumor-bearing mice with heparanase-inhibiting compounds, markedly attenuate tumor progression further underscoring the potential of anti-heparanase therapy for multiple types of cancer...
November 2016: Drug Resistance Updates: Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy
https://www.readbyqxmd.com/read/27911886/high-temperature-magnetism-and-microstructure-of-ferromagnetic-alloy-si1-x-mn-x
#14
B A Aronzon, A B Davydov, A L Vasiliev, N S Perov, O A Novodvorsky, L S Parshina, M Yu Presniakov, E Lahderanta
The results of a detailed study of magnetic properties and of the microstructure of SiMn films with a small deviation from stoichiometry are presented. The aim was to reveal the origin of the high temperature ferromagnetic ordering in such compounds. Unlike SiMn single crystals with the Curie temperature ~30 K, considered Si1-x Mn x compounds with x  =  0.5  +Δx and Δx in the range of 0.01-0.02 demonstrate a ferromagnetic state above room temperature. Such a ferromagnetic state can be explained by the existence of highly defective B20 SiMn nanocrystallites...
December 2, 2016: Journal of Physics. Condensed Matter: An Institute of Physics Journal
https://www.readbyqxmd.com/read/27911835/two-crystal-structures-reveal-design-for-repurposing-the-c-ala-domain-of-human-alars
#15
Litao Sun, Youngzee Song, David Blocquel, Xiang-Lei Yang, Paul Schimmel
The 20 aminoacyl tRNA synthetases (aaRSs) couple each amino acid to their cognate tRNAs. During evolution, 19 aaRSs expanded by acquiring novel noncatalytic appended domains, which are absent from bacteria and many lower eukaryotes but confer extracellular and nuclear functions in higher organisms. AlaRS is the single exception, with an appended C-terminal domain (C-Ala) that is conserved from prokaryotes to humans but with a wide sequence divergence. In human cells, C-Ala is also a splice variant of AlaRS...
November 28, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911826/structural-insights-into-the-lcib-protein-family-reveals-a-new-group-of-%C3%AE-carbonic-anhydrases
#16
Shengyang Jin, Jian Sun, Tobias Wunder, Desong Tang, Asaph B Cousins, Siu Kwan Sze, Oliver Mueller-Cajar, Yong-Gui Gao
Aquatic microalgae have evolved diverse CO2-concentrating mechanisms (CCMs) to saturate the carboxylase with its substrate, to compensate for the slow kinetics and competing oxygenation reaction of the key photosynthetic CO2-fixing enzyme rubisco. The limiting CO2-inducible B protein (LCIB) is known to be essential for CCM function in Chlamydomonas reinhardtii To assign a function to this previously uncharacterized protein family, we purified and characterized a phylogenetically diverse set of LCIB homologs...
December 1, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27911737/the-conservation-of-phosphate-binding-residues-among-pht1-transporters-suggests-that-distinct-transport-affinities-are-unlikely-to-result-from-differences-in-the-phosphate-binding-site
#17
REVIEW
S Antony Ceasar, Alison Baker, Stephen P Muench, S Ignacimuthu, Stephen A Baldwin
The plant PHosphate Transporter 1 (PHT1) family of membrane proteins belongs to the major facilitator super family and plays a major role in the acquisition of inorganic phosphate (Pi) from the soil and its transport within the plant. These transporters have been well characterized for expression patterns, localization, and in some cases affinity. Furthermore, the crystal structure of a high-affinity eukaryotic phosphate transporter from the fungus Piriformospora indica (PiPT) has revealed important information on the residues involved in Pi transport...
October 15, 2016: Biochemical Society Transactions
https://www.readbyqxmd.com/read/27911377/hybrid-cut-an-improved-sectioning-method-for-recalcitrant-plant-tissue-samples
#18
Tien-Kuan Chen, Hui-Ting Yang, Su-Chiung Fang, Yi-Chen Lien, Ting-Ting Yang, Swee-Suak Ko
Maintaining plant section integrity is essential for studying detailed anatomical structures at the cellular, tissue, or even organ level. However, some plant cells have rigid cell walls, tough fibers and crystals (calcium oxalate, silica, etc.), and high water content that often disrupt tissue integrity during plant tissue sectioning. This study establishes a simple Hybrid-Cut tissue sectioning method. This protocol modifies a paraffin-based sectioning technique and improves the integrity of tissue sections from different plants...
November 23, 2016: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/27910950/human-antibody-3e1-targets-the-ha-stem-region-of-h1n1-and-h5n6-influenza-a-viruses
#19
Wenshuai Wang, Xiaoyu Sun, Yanbing Li, Jinpeng Su, Zhiyang Ling, Tianlong Zhang, Fang Wang, Hong Zhang, Hualan Chen, Jianping Ding, Bing Sun
As influenza A viruses remain a major threat to human health worldwide, the discovery of broadly neutralizing monoclonal antibodies that recognize conserved epitopes would facilitate the development of antibody-based therapeutic strategies. Here we report that a VH4-4-encoded human mAb named 3E1 could neutralize H1 and H5 subtype viruses in vitro and protect mice against the H1N1 and H5N6 viruses by inhibiting the low pH-induced conformational rearrangement of haemagglutinin (HA), hence blocking membrane fusion...
December 2, 2016: Nature Communications
https://www.readbyqxmd.com/read/27910932/oer-activity-manipulated-by-iro6-coordination-geometry-an-insight-from-pyrochlore-iridates
#20
Wei Sun, Ji-Yuan Liu, Xue-Qing Gong, Waqas-Qamar Zaman, Li-Mei Cao, Ji Yang
The anodic reaction of oxygen evolution reaction (OER), an important point for electrolysis, however, remains the obstacle due to its complicated reaction at electrochemical interfaces. Iridium oxide (IrO2) is the only currently known 5d transition metal oxide possessing admirable OER activity. Tremendous efforts have been carried out to enhance the activity of iridium oxides. Unfortunately there lies a gap in understanding what factors responsible for the activity in doped IrO2 or the novel crystal structure...
December 2, 2016: Scientific Reports
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