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https://www.readbyqxmd.com/read/27933736/structural-insight-into-the-anti-prion-compound-inhibition-mechanism-of-native-prion-folding-over-misfolding
#1
Jiwon Choi, Rajiv Gandhi Govindaraj, Jae Wook Hyeon, Kyungro Lee, SongLing Ma, Su Yeon Kim, Jeongmin Lee, Kyoung Tai No
Transition of a physiological folded prion (PrP(C) ) into a pathogenic misfolded prion (PrP(S)(c) ) causes lethal neurodegenerative disorders and prion diseases. Anti-prion compounds have been developed to prevent this conversion; however, their mechanism of action remains unclear. Recently, we reported two anti-prion compounds, BMD29 and 35, identified by in silico and in vitro screening. In this study, we used extensive explicit-solvent molecular dynamics simulations to investigate ligand binding inhibition by anti-prion compounds in prion folding over misfolding behavior at acidic pH...
December 9, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27933735/danazol-has-potential-to-cause-pkc-translocation-cell-cycle-dysregulation-and-apoptosis-in-breast-cancer-cells
#2
Suman Jyoti Deka, Ashalata Roy, Vibin Ramakrishnan, Debasis Manna, Vishal Trivedi
Danazol, the established clinical drug has given promising therapeutic results in a series of clinical trials with breast cancer patients. Danazol shares structural similarities with several known PKC agonists and fits well into the C1 domain. Danazol binds to the C1b domain of PKC with Kd of 5.64±1.27 μM. MD simulation studies further support that the PKC-Danazol molecular model is stable and showing minimum distortion to the structure during the simulation period. Immunofluorescence and western-blotting studies indicate that MDAMB-231 cells stimulated with danazol exhibit translocation of PKCα to the plasma membrane...
December 9, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27933730/reactivity-of-9-aminoacridine-drug-quinacrine-with-glutathione-limits-its-anti-prion-activity
#3
Martin Šafařík, Tibor Moško, Zbigniew Zawada, Eva Šafaříková, Martin Dračínský, Karel Holada, Jaroslav Šebestík
Quinacrine - the drug based on 9-aminoacridine - failed in clinical trials for prion diseases, whereas it was active in in-vitro studies. We hypothesize that aromatic nucleophilic substitution at C9 could be contributing factor responsible for this failure because of the transfer of acridine moiety from quinacrine to abundant glutathione. Here, we described the semi-large-scale synthesis of the acridinylated glutathione and the consequences of its formation on biological and biophysical activities. The acridinylated glutathione is one order of magnitude weaker prion protein binder than the parent quinacrine...
December 9, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27933724/comparative-analysis-reveals-amino-acids-critical-for-anticancer-activity-of-peptide-cigb-552
#4
Soledad Astrada, Yolanda Gomez, Exequiel Barrera, Gonzalo Obal, Otto Pritsch, Sergio Pantano, Maribel G Vallespí, Mariela Bollati-Fogolín
Because of resistance development by cancer cells against current anticancer drugs, there is a considerable interest in developing novel antitumor agents. We have previously demonstrated that CIGB-552, a novel cell-penetrating synthetic peptide, was effective in reducing tumor size and increasing lifespan in tumor-bearing mice. Studies of protein-peptide interactions have shown that COMMD1 protein is a major mediator of CIGB-552 antitumor activity. Furthermore, a typical serine-protease degradation pattern for CIGB-552 in BALB/c mice serum was identified, yielding peptides which differ from CIGB-552 in size and physical properties...
November 2016: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/27933673/a-biophysical-and-computational-study-unraveling-the-molecular-interaction-mechanism-of-a-new-janus-kinase-inhibitor-tofacitinib-with-bovine-serum-albumin
#5
Ali Saber Abdelhameed, Saima Nusrat, Mohammad Rehan Ajmal, Syed Mohammad Zakariya, Masihuz Zaman, Rizwan Hasan Khan
The interaction of a recently certified kinase inhibitor Tofacitinib (TFB) with bovine serum albumin (BSA) has been studied, by spectroscopic and molecular docking studies. Spectrofluorimetric measurements at 3 different temperatures (288, 298, and 310 K) showed that TFB quench the intrinsic fluorescence of BSA upon forming a nonfluorescent complex. The intrinsic fluorescence data showed that TFB binds to BSA with binding constant (Kb ) of approximately 10(4) M(-1) , affirming a significant affinity of TFB with BSA...
December 9, 2016: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/27933619/monocyte-mediated-activation-of-endothelial-cells-occurs-only-after-binding-to-extracellular-vesicles-from-red-blood-cell-products-a-process-mediated-by-%C3%AE-integrin
#6
Marleen Straat, Maike E van Hezel, Anita Böing, Anita Tuip-De Boer, Nina Weber, Rienk Nieuwland, Robin van Bruggen, Nicole P Juffermans
BACKGROUND: Red blood cell (RBC) transfusion is associated with organ failure. The mechanism remains unknown, but may include adherence of blood cells to the microvasculature. We hypothesized that RBC-derived extracellular vesicles (EVs) interact with monocytes to activate endothelial cells. STUDY DESIGN AND METHODS: Human umbilical vein endothelial cells were incubated with supernatant from fresh and stored RBC units either containing EVs or depleted from EVs, with or without the addition of immune cells...
December 2016: Transfusion
https://www.readbyqxmd.com/read/27933547/anti-neuroinflammatory-effects-of-fucoxanthin-via-inhibition-of-akt-nf-%C3%AE%C2%BAb-and-mapks-ap-1-pathways-and-activation-of-pka-creb-pathway-in-lipopolysaccharide-activated-bv-2-microglial-cells
#7
Dong Zhao, Seung-Hwan Kwon, Yoon Sun Chun, Ming-Yao Gu, Hyun Ok Yang
Microglia play a critical role in controlling the homeostasis of the brain, but over-activated microglia secrete pro-inflammatory mediators and cytokines, which induce neuronal cell death. Fucoxanthin (Fx), a marine carotenoid, has demonstrated a variety of beneficial health effects. Despite accumulating evidence supporting the immune-modulating effects of Fx in vitro, the underlying signaling pathways remain unknown. In the present study, Fx dose-dependently inhibited the secretion of lipopolysaccharide (LPS)-induced pro-inflammatory mediators including interleukin (IL)-6, tumor necrosis factor (TNF)-α, reactive oxygen species (ROS), prostaglandin (PG) E2, and nitric oxide (NO) productions, and also suppressed the expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 enzymes...
December 8, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27933517/a-novel-mutation-in-the-fibrinogen-a%C3%AE-chain-gly13arg-fibrinogen-nanning-causes-congenital-dysfibrinogenemia-associated-with-defective-peptide-a-release
#8
Jie Yan, Meiling Luo, Peng Cheng, Lin Liao, Xuelian Deng, Donghong Deng, Faquan Lin
Dysfibrinogenemia is characterized by blood coagulation dysfunction induced by an abnormal molecular structure of fibrinogen. Here, we describe a new case. A 32-year-old female was suspected of having dysfibrinogenemia during routine laboratory screening, based on her decreased functional fibrinogen level, normal fibrinogen antigen level, and prolonged thrombin time. We extracted DNA and performed polymerase chain reaction and DNA sequencing to identify genetic mutation. Fibrin polymerization, the kinetics of the fibrinopeptide release, scanning electron microscopy, mass spectrometric analysis, fibrin cross-linking, sodium dodecyl sulfate polyacrylamide gel electrophoresis and western blot were conducted...
December 8, 2016: International Journal of Hematology
https://www.readbyqxmd.com/read/27933513/effect-of-yiqi-tongyang-decoction-on-blood-t-cell-subsets-in-patients-with-chronic-immune-thrombocytopenia
#9
Xiu-Peng Yang, Rou Ma, Xiao-Hong Yang, Hui-Lan Zhu, Yong-Gang Xu
OBJECTIVE: To measure the proportions of blood T cell subsets, Th1, Th2, Th17, Th22, and Treg cells, and other parameters in patients with chronic immune thrombocytopenia (CITP) before and after treatment with Yiqi Tongyang Decoction (, YTD) to explore T cell status of patients with CITP, and to define the mechanism of action of YTD. METHODS: The changes in peripheral blood T lymphocyte subsets, and those of Th1, Th2, Th17, Th22, and Treg cells in 30 patients with CITP (22 females and 8 males) were analyzed using multiparametric flow cytometry before and after treatment with YTD for 6 months, and 26 healthy volunteers (14 males and 12 females) acted as a control...
December 9, 2016: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/27933499/assessment-of-molecularly-imprinted-polymers-mips-in-the-preconcentration-of-disperse-red-73-dye-prior-to-photoelectrocatalytic-treatment
#10
Jefferson Honorio Franco, Alejandra Ben Aissa, Guilherme Garcia Bessegato, Laura Martinez Fajardo, Maria Valnice Boldrin Zanoni, María Isabel Pividori, Maria Del Pilar Taboada Sotomayor
Magnetic molecularly imprinted polymers (MMIPs) have become a research hotspot due to their two important characteristics: target recognition and magnetic separation. This paper presents the preparation, characterization, and optimization of an MMIP for the preconcentration of disperse red 73 dye (DR73) and its subsequent efficient degradation by photoelectrocatalytic treatment. The MMIPs were characterized by scanning electron microscopy (SEM), which revealed homogeneous distribution of the particles. Excellent encapsulation of magnetite was confirmed by transmission electron microscopy (TEM)...
December 8, 2016: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/27933484/dna-as-a-target-for-anticancer-phen-imidazole-pd-ii-complexes
#11
Maryam Heydari, Mahboube Eslami Moghadam, AliAkbar Tarlani, Hossein Farhangian
Imidazole ring is a known structure in many natural or synthetic drug molecules and its metal complexes can interact with DNA and do the cleavage. Hence, to study the influence of the structure and size of the ligand on biological behavior of metal complexes, two water-soluble Pd(II) complexes of phen and FIP ligands (where phen is 1,10-phenanthroline and FIP is 2-(Furan-2-yl)-1H-Imidazo[4,5-f][1, 10]phenanthroline) with the formula of [Pd(phen)(FIP)](NO3)2 and [Pd(FIP)2]Cl2, that were activated against chronic myelogenous leukemia cell line, K562, were selected...
December 8, 2016: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/27933483/covalent-immobilization-of-human-placental-17%C3%AE-hydroxysteroid-dehydrogenase-type-1-onto-glutaraldehyde-activated-silica-coupled-with-lc-tof-ms-for-anti-cancer-drug-screening-applications
#12
Yin Bai, Wen-Di Zhou, Xian-Min Mu, Qian Zhang, Chen Yu, Bin Di, Meng-Xiang Su
Human 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), a potential target in breast cancer prevention and therapy, was extracted from human placenta and immobilized on nonporous silica (∼5 μm) with a covalent method for the first time. The optimum initial enzyme concentration and immobilization time during the immobilization process were 0.42 mg mL(-1) and 12 h, repectively. The binding was confirmed by scanning electron microscope (SEM) and infrared spectroscopy (FT-IR). It could improve the pH, thermal and storage stability compared to free enzyme...
December 8, 2016: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/27933470/erratum-to-identification-of-a-novel-binding-protein-of-fat10-eukaryotic-translation-elongation-factor-1a1
#13
Xin Yu, Xiuxia Liu, Tiande Liu, Kui Hong, Jun Lei, Rongfa Yuan, Jianghua Shao
No abstract text is available yet for this article.
December 8, 2016: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/27933466/microrna-145-modulates-epithelial-mesenchymal-transition-and-suppresses-proliferation-migration-and-invasion-by-targeting-sip1-in-human-cervical-cancer-cells
#14
Anusha Sathyanarayanan, Karthik Subramanian Chandrasekaran, Devarajan Karunagaran
PURPOSE: Previously, it has been reported that microRNA-145 (miR-145) is lowly expressed in human cervical cancers and that its putative tumour suppressive role may be attributed to epithelial-mesenchymal transition (EMT) regulation. Here, we aimed to assess whether miR-145 may affect EMT-associated markers/genes and suppress cervical cancer growth and motility, and to provide a mechanistic basis for these phenomena. METHODS: The identification of the SMAD-interacting protein 1 (SIP1) mRNA as putative miR-145 target was investigated using a 3' untranslated region (3'UTR) luciferase assay and Western blotting, respectively...
December 8, 2016: Cellular Oncology (Dordrecht)
https://www.readbyqxmd.com/read/27933445/correlation-of-crevicular-fluid-and-serum-levels-of-retinol-binding-protein-4-and-leptin-in-chronic-periodontitis-and-obesity
#15
Dharmendra Kanoriya, A R Pradeep, A Mallika, Sandeep Singhal, Vibhuti Garg
OBJECTIVE: Retinol-binding protein 4 (RBP4) and leptin are both adipokines and involved in the pathophysiology of different vascular and inflammatory diseases and selectively elevated in patients with obesity. The aim of the present study was to determine and correlate the levels of RBP4 and leptin in gingival crevicular fluid (GCF) and serum in patients with chronic periodontitis (CP) and obesity. MATERIALS AND METHODS: A total of 70 patients with age group 25 to 45 years were divided into four groups based on gingival index (GI), probing depth (PD), clinical attachment level (CAL), body mass index (BMI) and radiographic evidence of bone loss...
December 8, 2016: Clinical Oral Investigations
https://www.readbyqxmd.com/read/27933426/characterization-of-the-first-fully-human-anti-tem1-scfv-in-models-of-solid-tumor-imaging-and-immunotoxin-based-therapy
#16
Xiaopeng Yuan, Mingjuan Yang, Xiang Chen, Xuhua Zhang, Shrey Sukhadia, Najia Musolino, Huijing Bao, Tingtao Chen, Chen Xu, Qirui Wang, Stephen Santoro, Daniel Ricklin, Jia Hu, Ruihe Lin, Wei Yang, Zhijun Li, Weijun Qin, Aizhi Zhao
Tumor endothelial marker 1 (TEM1) has been identified as a novel surface marker upregulated on the blood vessels and stroma in many solid tumors. We previously isolated a novel single-chain variable fragment (scFv) 78 against TEM1 from a yeast display scFv library. Here, we evaluated the potential applications of scFv78 as a tool for tumor molecular imaging, immunotoxin-based therapy and nanotherapy. Epitope mapping, three-dimensional structure docking and affinity measurements indicated that scFv78 could bind to both human and murine TEM1, with equivalent affinity, at a well-conserved conformational epitope...
December 8, 2016: Cancer Immunology, Immunotherapy: CII
https://www.readbyqxmd.com/read/27933395/influence-of-the-her-receptor-ligand-system-on-sensitivity-to-cetuximab-and-trastuzumab-in-gastric-cancer-cell-lines
#17
Julia Kneissl, Anja Hartmann, Nicole Pfarr, Franziska Erlmeier, Thomas Lorber, Simone Keller, Gwen Zwingenberger, Wilko Weichert, Birgit Luber
PURPOSE: Gastric cancer remains a major health concern, and improvement of the therapeutic options is crucial. Treatment with targeted therapeutics such as the EGFR-targeting antibody cetuximab or the HER2-targeting antibody trastuzumab is either ineffective or moderately effective in this disease, respectively. In this study, we analysed the involvement of the HER receptor ligands amphiregulin (AREG), epidermal growth factor (EGF), heparin-binding epidermal growth factor (HB-EGF) and transforming growth factor alpha (TGFα) in the responsiveness of gastric cancer cell lines to cetuximab and trastuzumab...
December 8, 2016: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/27933291/endocytosis-and-physiology-insights-from-disabled-2-deficient-mice
#18
REVIEW
Wensi Tao, Robert Moore, Elizabeth R Smith, Xiang-Xi Xu
Disabled-2 (Dab2) is a clathrin and cargo binding endocytic adaptor protein, and cell biology studies revealed that Dab2 plays a role in cellular trafficking of a number of transmembrane receptors and signaling proteins. A PTB/PID domain located in the N-terminus of Dab2 binds the NPXY motif(s) present at the cytoplasmic tails of certain transmembrane proteins/receptors. The membrane receptors reported to bind directly to Dab2 include LDL receptor and its family members LRP1 and LRP2 (megalin), growth factor receptors EGFR and FGFR, and the cell adhesion receptor beta1 integrin...
2016: Frontiers in Cell and Developmental Biology
https://www.readbyqxmd.com/read/27933274/screening-and-identification-of-an-h-2k-b-restricted-ctl-epitope-within-the-glycoprotein-of-hantaan-virus
#19
Rui-Xue Ma, Lin-Feng Cheng, Qi-Kang Ying, Rong-Rong Liu, Tie-Jun Ma, Xiao-Xiao Zhang, Zi-Yu Liu, Liang Zhang, Wei Ye, Fang-Lin Zhang, Zhi-Kai Xu, Fang Wang, Xing-An Wu
The cytotoxic T lymphocyte (CTL) response plays a key role in controlling viral infection, but only a few epitopes within the HTNV glycoprotein (GP) that are recognized by CTLs have been reported. In this study, we identified one murine HTNV GP-derived H2-K(b)-restricted CTL epitope in C57BL/6 mice, which could be used to design preclinical studies of vaccines for HTNV infection. First, 15 8-mer peptides were selected from the HTNV GP amino acid sequence based on a percentile rank of <=1% by IEDB which is the most comprehensive collection of epitope prediction and analysis tool...
2016: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/27933225/rational-design-of-dual-active-sites-in-a-single-protein-scaffold-a-case-study-of-heme-protein-in-myoglobin
#20
Xiao-Gang Shu, Ji-Hu Su, Ke-Jie Du, Yong You, Shu-Qin Gao, Ge-Bo Wen, Xiangshi Tan, Ying-Wu Lin
Rational protein design has been proven to be a powerful tool for creating functional artificial proteins. Although many artificial metalloproteins with a single active site have been successfully created, those with dual active sites in a single protein scaffold are still relatively rare. In this study, we rationally designed dual active sites in a single heme protein scaffold, myoglobin (Mb), by retaining the native heme site and creating a copper-binding site remotely through a single mutation of Arg118 to His or Met...
June 2016: ChemistryOpen
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