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https://www.readbyqxmd.com/read/28340074/synthetic-human-neutrophil-peptide-1-inhibits-platelet-adhesion-and-aggregation-on-von-willebrand-factor-collagen-surface-under-arterial-shear-stress-through-disulfide-bond-reduction-mechanism
#1
Jenny McDaniel, X Long Zhen
No abstract text is available yet for this article.
March 1, 2017: American Journal of Clinical Pathology
https://www.readbyqxmd.com/read/28338927/the-effect-of-aluminum-ion-on-the-aggregation-of-human-islet-amyloid-polypeptide-11-28
#2
Lanlan Su, Cheng Lu, Peng Yan, Nan Zhang, Sheng Cai, Gongjun Zhang, Xingfei Zhou, Bin Li
Metal ions play a critical role in human islet amyloid polypeptide (hIAPP) aggregation, which is believed to be closely associated with β-cell death in type II diabetes. In this work, the effect of Al3+ on the aggregation of hIAPP (11-28) was studied by several different experimental approaches. Atomic force microscopy measurements showed that Al3+ could remarkably inhibit hIAPP(11-28) fibrillogenesis, while Zn2+ had a slight promotion effect on peptide aggregation, which was also confirmed by Thioflavin T fluorescence observation...
March 10, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28338415/hyaluronic-acid-hydrogel-functionalized-with-self-assembled-micelles-of-amphiphilic-pegylated-kartogenin-for-the-treatment-of-osteoarthritis
#3
Mi-Lan Kang, Se-Young Jeong, Gun-Il Im
Synthetic hyaluronic acid (HA) containing a covalently integrated drug is capable of releasing therapeutic molecules and is an attractive candidate for the intra-articular treatment of osteoarthritis (OA). Herein, self-assembled PEGylated kartogenin (PEG/KGN) micelles consisting of hydrophilic polyethylene glycol (PEG) and hydrophobic KGN, which has been shown to induce chondrogenesis in human mesenchymal stem cells, were prepared by covalent crosslinking. HA hydrogels containing PEG/KGN micelles (HA/PEG/KGN) were prepared by covalently bonding PEG chains to HA...
March 24, 2017: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/28335566/profiling-and-preparation-of-metabolites-from-pyragrel-in-human-urine-by-online-solid-phase-extraction-coupled-with-high-performance-liquid-chromatography-tandem-mass-spectrometry-followed-by-a-macroporous-resin-based-purification-approach
#4
Xin Zhao, Jingjing Jiang, Guang Yang, Jie Huang, Guoping Yang, Guangwei He, Zhaoxing Chu, Taijun Hang, Guorong Fan
Pyragrel, a new anticoagulant drug, is derived from the molecular combination of ligustrazine and ferulic acid. Pyragrel showed significant inhibitory activity against platelet aggregation induced by adenosine diphosphate (ADP), and had been approved for a phase I clinical trial by CFDA. To characterize the metabolites of Pyragrel in human urine after intravenous administration, a reliable online solid-phase extraction couple with high performance liquid chromatography tandem mass spectrometry (online SPE-HPLC-MS(n)) method was conceived and applied...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334993/the-mechanism-of-the-glycosylase-reaction-with-hogg1-base-excision-repair-enzyme-concerted-effect-of-lys249-and-asp268-during-excision-of-8-oxoguanine
#5
Jakub Šebera, Yoshikazu Hattori, Daichi Sato, David Reha, Radim Nencka, Takashi Kohno, Chojiro Kojima, Yoshiyuki Tanaka, Vladimír Sychrovský
The excision of 8-oxoguanine (oxoG) by the human 8-oxoguanine DNA glycosylase 1 (hOGG1) base-excision repair enzyme was studied by using the QM/MM (M06-2X/6-31G(d,p):OPLS2005) calculation method and nuclear magnetic resonance (NMR) spectroscopy. The calculated glycosylase reaction included excision of the oxoG base, formation of Lys249-ribose enzyme-substrate covalent adduct and formation of a Schiff base. The formation of a Schiff base with ΔG# = 17.7 kcal/mol was the rate-limiting step of the reaction. The excision of the oxoG base with ΔG# = 16...
March 6, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28332820/kinetic-landscape-of-a-peptide-bond-forming-prolyl-oligopeptidase
#6
Clarissa Melo Czekster, James H Naismith
Prolyl oligopeptidase B from Galerina marginata (GmPOPB) has recently been discovered as a peptidase capable of breaking and forming peptide bonds to yield a cyclic peptide. Despite the relevance of prolyl oligopeptidases in human biology and disease, a kinetic analysis pinpointing rate-limiting steps for a member of this enzyme family is not available. Macrocyclase enzymes are currently exploited to produce cyclic peptides with potential therapeutic applications. Cyclic peptides are promising drug-like molecules due to their stability and conformational rigidity...
March 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28330134/phytases-from-enterobacter-and-serratia-species-with-desirable-characteristics-for-food-and-feed-applications
#7
Harpreet Kaur Kalsi, Rajveer Singh, Harcharan Singh Dhaliwal, Vinod Kumar
Phytases are enzymes of great industrial importance with wide range of applications in animal and human nutrition. These catalyze the hydrolysis of phosphomonoester bonds in phytate, thereby releasing lower forms of myo-inositol phosphates and inorganic phosphate. Addition of phytase to plant-based foods can improve its nutritional value and increase mineral bioavailability by decreasing nutritional effect of phytate. In the present investigation, 43 phytase positive bacteria on PSM plates were isolated from different sources and characterized for phytase activity...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28327441/structure-based-design-synthesis-and-biological-evaluation-of-amino-phosphonate-derivatives-as-human-glucokinase-activators
#8
Nanda Kumar Yellapu, Ravendra Babu Kilaru, Nagaraju Chamarthi, Sarma Pvgk, Bhaskar Matcha
Glucokinase (GK) is a potential therapeutic target of type 2 diabetes and GK activators (GKAs) represent a promising class of small organic molecules which enhance GK activity. Based on the configuration and conformation of the allosteric site of GK, we have designed a novel class of amino phosphonate derivatives in order to develop potent GKAs. The QSAR model developed using numerous descriptors revealed its potential with the best effective statistical values of RMSE=1.52 and r(2)=0.30. Moreover, application of this model on the present test set GKAs proved to be worthy to predict their activities as a better linear relationship was observed with RMSE=0...
March 2, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28327437/evaluating-the-effect-of-antioxidant-agents-on-shear-bond-strength-of-tooth-colored-restorative-materials-after-bleaching-a-systematic-review
#9
REVIEW
Atiyeh Feiz, Hamid Mosleh, Rahman Nazeri
PURPOSE: The main objective of the present study was to make a systematic review of how antioxidant agents affect shear bond strength of tooth-colored restorative materials after bleaching. DATA SOURCES: Electronic search was used to extract the related articles on the targeted key words such as "antioxidant", "dental bleaching" and "shear bond strength" (SBS) from MeSH, PubMed, Medline, and Cochrane electronic data bases. These articles were all published before 2016...
March 10, 2017: Journal of the Mechanical Behavior of Biomedical Materials
https://www.readbyqxmd.com/read/28326775/determining-cysteines-available-for-covalent-inhibition-across-the-human-kinome
#10
Zheng Zhao, Qingsong Liu, Spencer Bliven, Lei Xie, Philip E Bourne
Covalently bound protein kinase inhibitors have been frequently designed to target non-catalytic cysteines at the ATP binding site. Thus, it is important to know if a given cysteine can form a covalent bond. Here we combine a function-site interaction fingerprint method and DFT calculations to determine the potential of cysteines to form a covalent interaction with an inhibitor. By harnessing the human structural kinome, a comprehensive structure-based binding site cysteine dataset was assembled. The orientation of the cysteine thiol group indicates which cysteines can potentially form covalent bonds...
March 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28326226/comparison-of-four-methods-for-the-biofunctionalization-of-gold-nanorods-by-the-introduction-of-sulfhydryl-groups-to-antibodies
#11
Xuefeng Wang, Zhong Mei, Yanyan Wang, Liang Tang
Introducing sulfhydryl groups to biomolecules to functionalize gold nanorods (GNRs) is an attractive method that involves the creation of a strong Au-S bond. Previously, we developed a facile method to functionalize GNR surfaces by thiolating antibodies using Traut's reagent. In the current study, we evaluated several methods for the introduction of thiol groups onto the surface of GNRs by using Traut's reagent, dithiotreitol (DTT), dithiolaromatic PEG6-CONHNH2, and thiol-polyethylene glycolamine (SH-PEG-NH2) combined with EDC reaction...
2017: Beilstein Journal of Nanotechnology
https://www.readbyqxmd.com/read/28325601/design-and-synthesis-of-novel-6-aryl-substituted-4-anilinequinazoline-derivatives-as-potential-pi3k%C3%AE-inhibitors
#12
Minhang Xin, Yuan-Yuan Hei, Hao Zhang, Ying Shen, San-Qi Zhang
In this study, a series of new 6-aryl substituted 4-anilinequinazolines was designed and synthesized as PI3Kδ inhibitors based on our reported chemical structures. The preliminary structure-activity relationship (SAR) was established, and compounds 13h and 13k displayed most potent PI3Kδ inhibitory activities with the IC50 values of 9.3nM and 9.7nM, respectively. Compound 13h demonstrated similar anti-proliferative profiles to idelalisib against three human B cell lines. Three key hydrogen bonding interactions were found in the docking of 13h with PI3Kδ enzyme...
March 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28323167/high-hydrostatic-pressure-enables-almost-100-refolding-of-recombinant-human-ciliary-neurotrophic-factor-from-inclusion-bodies-at-high-concentration
#13
Qi Wang, Yongdong Liu, Chun Zhang, Fangxia Guo, Cui Feng, Xiunan Li, Hong Shi, Zhiguo Su
Protein refolding from inclusion bodies (IBs) often encounters a problem of low recovery at high protein concentration. In this study, we demonstrated that high hydrostatic pressure (HHP) could simultaneously achieve high refolding concentration and high refolding yield for IBs of recombinant human ciliary neurotrophic factor (rhCNTF), a potential therapeutic for neurodegenerative diseases. The use of dilution refolding obtained 18% recovery at 3 mg/mL, even in the presence of 4 M urea. In contrast, HHP refolding could efficiently increase the recovery up to almost 100% even at 4 mg/mL...
March 18, 2017: Protein Expression and Purification
https://www.readbyqxmd.com/read/28321700/thermoactivated-persulfate-oxidation-of-pesticide-chlorpyrifos-in-aquatic-system-kinetic-and-mechanistic-investigations
#14
Lei Zhou, Ya Zhang, Rongrong Ying, Guoqing Wang, Tao Long, Jianhua Li, Yusuo Lin
The widespread occurrence of organophosphorus pesticides (OPPs) in the environment poses risks to both ecologic system as well as human health. This study investigated the oxidation kinetics of chlorpyrifos (CP), one of the typical OPPs, by thermoactivated persulfate (PS) oxidation process, and evaluated the influence of key kinetic factors, such as PS concentrations, pH, temperature, bicarbonate, and chloride ions. The reaction pathways and mechanisms were also proposed based on products identification by LC-MS techniques...
March 20, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28319523/plasma-levels-of-microrna-155-are-upregulated-with-long-term-left-ventricular-assist-device-support
#15
Teresa Wang, Emily C OʼBrien, Joseph G Rogers, Daniel L Jacoby, Michael E Chen, Jeffrey M Testani, Dawn E Bowles, Carmelo A Milano, G Michael Felker, Chetan B Patel, Pramod N Bonde, Tariq Ahmad
Left ventricular assist device (LVAD) therapy unloads the failing heart but exposes the human body to unique pathophysiological demands such as continuous blood-flow and complete univentricular support, which are associated with increased risk of adverse clinical outcomes. MiRNAs are 22-23 nucleotide RNAs involved in regulation of multiple biological processes including the pathogenesis of heart failure (HF). Thus, measurement of miRNAs may have potential in both diagnostics as circulating biomarkers, and in therapeutics for targeted interventions...
March 17, 2017: ASAIO Journal: a Peer-reviewed Journal of the American Society for Artificial Internal Organs
https://www.readbyqxmd.com/read/28318221/crystal-structure-of-a-homogeneous-igg-fc-glycoform-with-the-n-glycan-designed-to-maximize-the-antibody-dependent-cellular-cytotoxicity
#16
Chia-Lin Chen, Jen-Chi Hsu, Chin-Wei Lin, Chia-Hung Wang, Ming-Hung Tsai, Chung-Yi Wu, Chi-Huey Wong, Che Ma
N-glycosylation on IgG modulates Fc conformation and effector functions. An IgG-Fc contains a human sialo-complex type (hSCT) glycan of biantennary structure with two α2,6-sialylations and without core-fucosylation is an optimized glycoform developed to enhance the antibody dependent cellular cytotoxicity (ADCC). hSCT modification not only enhances the binding affinity to Fc receptors in the presence of antigen, but also in some cases provides gain-of-function effector activity. We used enzymatic glyco-engineering to prepare an IgG-Fc with homogeneous hSCT attached to each CH2 domain, and solved its crystal structure...
March 20, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28317948/local-remodeling-of-synthetic-extracellular-matrix-microenvironments-by-co-cultured-endometrial-epithelial-and-stromal-cells-enables-long-term-dynamic-physiological-function
#17
Christi D Cook, Abby S Hill, Margaret Guo, Linda Stockdale, Julia P Papps, Keith B Isaacson, Douglas A Lauffenburger, Linda G Griffith
Mucosal barrier tissues, comprising a layer of tightly-bonded epithelial cells in intimate molecular communication with an underlying matrix-rich stroma containing fibroblasts and immune cells, are prominent targets for drugs against infection, chronic inflammation, and other disease processes. Although human in vitro models of such barriers are needed for mechanistic studies and drug development, differences in extracellular matrix (ECM) needs of epithelial and stromal cells hinder efforts to create such models...
March 20, 2017: Integrative Biology: Quantitative Biosciences From Nano to Macro
https://www.readbyqxmd.com/read/28317157/design-and-synthesis-of-novel-anti-plasmodial-histone-deacetylase-inhibitors-containing-an-alkoxyamide-connecting-unit
#18
Leandro A Alves Avelar, Jana Held, Jessica A Engel, Parichat Sureechatchaiyan, Finn K Hansen, Alexandra Hamacher, Matthias U Kassack, Benjamin Mordmüller, Katherine T Andrews, Thomas Kurz
Despite recent declines in mortality, malaria remains an important global health problem. New therapies are needed, including new drugs with novel modes of action compared to existing agents. Among new potential therapeutic targets for malaria, inhibition of parasitic histone deacetylases (HDACs) is a promising approach. Homology modeling of PfHDAC1, a known target of some anti-plasmodial HDAC inhibitors, revealed a unique threonine residue at the rim of the active site in close proximity to the location of the cap group of vorinostat-type HDAC inhibitors...
March 20, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28315768/peptide-protein-interactions-within-human-hair-keratins
#19
Célia F Cruz, Teresa Matamá, Artur Cavaco-Paulo
We selected 1235 decapeptides from human hair proteins encoded by human genes of keratins and keratin associated proteins. The peptides were linked to glass arrays and screened for their affinity towards a solution of human hair extracted keratin fraction. Based on the physicochemical properties of the peptides, ten variables were studied: content of different types of amino acid side chains (cysteine, hydrophobic, polar, basic, acidic, aromatic rings, amide, alcohol side chains), isoelectric point, and net charge...
March 15, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28315376/effect-of-a-novel-quaternary-ammonium-silane-cavity-disinfectant-on-durability-of-resin-dentine-bond
#20
D Umer, C K Y Yiu, M F Burrow, L-N Niu, F R Tay
OBJECTIVE: The present study examined the effect of a quaternary ammonium silane (QAS) cavity disinfectant on the viability of human dental pulp cells, dentine bond durability and nanoleakage of simplified etch-and-rinse adhesives. METHODS: Etched dentine surface of third molars were randomly divided into two adhesive groups, Adper™ Single Bond 2 and Prime & Bond(®) NT™. For each adhesive, the teeth were randomly assigned to five cavity disinfectant groups (N=6): Group 1: deionised water (control); Group 2: 2% chlorhexidine (CHX); Group 3: 2% QAS; Group 4: 5% QAS and Group 5: 10% QAS...
March 14, 2017: Journal of Dentistry
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