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https://www.readbyqxmd.com/read/28343375/foxo1-suppression-is-a-determinant-of-acquired-lapatinib-resistance-in-her2-positive-gastric-cancer-cells-through-met-upregulation
#1
Jinju Park, Yiseul Choi, Young San Ko, Younghoon Kim, Jung-Soo Pyo, Bo Gun Jang, Min A Kim, Jae-Seon Lee, Mee Soo Chang, Jong-Wan Park, Byung Lan Lee
Purpose: Lapatinib is a candidate drug for treatment of trastuzumab-resistant, HER2-positive gastric cancer (GC). Unfortunately, lapatinib resistance renders this drug ineffective. The present study investigated the implication of forkhead box protein O1 (FOXO1) signaling in the acquired lapatinib resistance in HER2-positive GC cells. Materials and Methods: Lapatinib-resistant GC cell lines (SNU-216 LR2-8) were generated in vitro by chronic exposure of lapatinib-sensitive, HER2-positive SNU-216 cells to lapatinib...
March 24, 2017: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/28343264/modulating-the-ph-activity-profiles-of-phenylalanine-ammonia-lyase-from-anabaena-variabilis-by-modification-of-center-near-surface-residues
#2
Fan Zhang, Nan Huang, Li Zhou, Wenjing Cui, Zhongmei Liu, Longbao Zhu, Yi Liu, Zhemin Zhou
Phenylalanine ammonia lyase from Anabaena variabilis (Av-PAL) is a candidate for the treatment of phenylketonuria (PKU). However, Av-PAL shows its optimal pH at 8.5 and maintains only 70% of its highest activity when pH decreases to 7.3-7.4 (the condition of human plasma). The objective of the study was to shift its optimal pH by mutating surface amino acid residues which interact with the general base Tyr78. Based on the crystal structure and the online program GETAREA, we selected five sites: Asn69, Glu72, Glu75, Asn89, and Val90...
March 25, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28343241/in-vitro-activity-of-alpha-mangostin-in-killing-and-eradicating-staphylococcus-epidermidis-rp62a-biofilms
#3
Murugesan Sivaranjani, Manivannan Prakash, Shanmugaraj Gowrishankar, Janarthanam Rathna, Shunmugiah Karutha Pandian, Arumugam Veera Ravi
Alpha-mangostin (α-MG) has been reported to be an effective antibacterial agent against planktonic cells of many Gram-positive bacteria. However, the antibiofilm potency of α-MG remains unexplored till date. In this study, the antibiofilm and mature biofilm eradication ability of α-MG against Staphylococcus epidermidis RP62A (ATCC 35984) biofilms were evaluated. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of α-MG against S. epidermidis RP62A were found to be 1...
March 25, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28343133/single-crystal-cr2o3-nanoplates-with-differing-crystalinities-derived-from-trinuclear-complexes-and-embedded-in-a-carbon-matrix-as-an-electrode-material-for-supercapacitors
#4
Jikui Zhu, Yuqian Jiang, Zhiyong Lu, Chenglan Zhao, Li Xie, Lingyun Chen, Jingui Duan
As one kind of important p-type semiconductors, Cr2O3 has been widely used for optical and electronic devices due to its high electrical conductivity and special optoelectronic characteristics, as well as high chemical and thermal stability. In this paper, single-crystalline Cr2O3 nanoplates embedded in carbon matrix were successfully synthesized through direct thermal decomposition of a trinuclear cluster complex of [Cr3O(CH3CO2)6(H2O)3]NO3·CH3COOH ([Cr3O]) in Ar atmosphere. The synergetic effect of the plate-like structure and embedding in carbon matrix contributes to the enhanced electrochemical performance of the Cr2O3-C nanoplates...
March 18, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28343125/structural-modeling-of-human-organic-cation-transporters
#5
Tikam Chand Dakal, Rajender Kumar, Dindial Ramotar
Human organic cation transporters (hOCTs) belong to solute carriers (SLC) 22 family of membrane proteins that play a central role in transportation of chemotherapeutic drugs for several clinical and pathological conditions, including cancer and diabetes. These transporters mediate drug transport; however, the precise mechanism of drug-binding and transport by them is not fully uncovered yet, partly due to unavailability of any crystal structure record. In this work, we performed a multi-phasic approach to compute the 3D structural models of seven human organic cation transporters (hOCTs) starting from primary protein sequence...
March 18, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28343118/real-time-formation-of-salivary-films-onto-polymeric-materials-for-dental-applications-differences-between-unstimulated-and-stimulated-saliva
#6
Florian Weber, Alejandro Barrantes
The formation of salivary films onto oral prostheses materials is of central importance for understanding their performance and interaction with oral tissue and flora. The aim of this work was to study and compare the salivary films formed from unstimulated and stimulated whole saliva on two common polymeric materials, polycarbonate and poly(methyl methacrylate). Irradiating these materials with UV light is a simple way to modify their wettability, roughness and ζ-potential. Therefore, the effect of UV exposure of polycarbonate and poly(methyl methacrylate) on saliva adsorption was also investigated...
March 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28343102/acoustic-and-hybrid-3d-printed-electrochemical-biosensors-for-the-real-time-immunodetection-of-liver-cancer-cells-hepg2
#7
Samar Damiati, Seta Küpcü, Martin Peacock, Christoph Eilenberger, Mazin Zamzami, Ishtiaq Qadri, Hani Choudhry, Uwe B Sleytr, Bernhard Schuster
This study presents an efficient acoustic and hybrid three-dimensional (3D)-printed electrochemical biosensors for the detection of liver cancer cells. The biosensors function by recognizing the highly expressed tumor marker CD133, which is located on the surface of liver cancer cells. Detection was achieved by recrystallizing a recombinant S-layer fusion protein (rSbpA/ZZ) on the surface of the sensors. The fused ZZ-domain enables immobilization of the anti-CD133 antibody in a defined manner. These highly accessible anti-CD133 antibodies were employed as a sensing layer, thereby enabling the efficient detection of liver cancer cells (HepG2)...
March 21, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28343050/photocatalytic-efficiency-of-fe2o3-tio2-for-the-degradation-of-typical-dyes-in-textile-industries-effects-of-calcination-temperature-and-uv-assisted-thermal-synthesis
#8
Mohsen Nasirian, Ciro Fernando Bustillo-Lecompte, Mehrab Mehrvar
The inadequate management practices in industrial textile effluents have a considerable negative impact on the environment and human health due to the indiscriminate release of dyes. Photocatalysis is one of the diverse advance oxidation processes (AOPs) and titanium dioxide (TiO2) is recognized for its high oxidation and reduction power. A composite photocatalyst of Fe2O3/TiO2 is synthesized using different mass ratios of Fe:TiO2 to improve its photoactivity. The composite photocatalyst is calcined at 300-900 °C...
March 23, 2017: Journal of Environmental Management
https://www.readbyqxmd.com/read/28342850/structural-basis-for-differential-activities-of-enantiomeric-ppar%C3%AE-agonists-binding-of-s35-to-the-alternate-site
#9
Jun Young Jang, Minseob Koh, Hwan Bae, Doo Ri An, Ha Na Im, Hyoun Sook Kim, Ji Young Yoon, Hye-Jin Yoon, Byung Woo Han, Seung Bum Park, Se Won Suh
Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, type 2 diabetes mellitus, and inflammation. Many PPARγ agonists bind to the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i.e., helix H12) of the ligand-binding domain (LBD). More recently, an alternate ligand-binding site was identified in PPARγ LBD; it is located beside the Ω loop between the helices H2' and H3...
March 22, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28342783/effect-of-storage-on-the-physical-stability-of-thin-polymethacrylate-perphenazine-films
#10
Kristiina Korhonen, Elina Smolander, Ossi Korhonen, Jarkko Ketolainen, Riikka Laitinen
We evaluated the physical stability of thin polymethacrylate-drug films under three different storage conditions by X-ray powder diffraction, differential scanning calorimetry, scanning electron microscopy, polarized light microscopy, and Fourier transform infrared spectroscopy. Mechanical properties i.e. elongation, mechanical strength, and in vitro drug release from the thin films were also determined during storage. The films consisted of ammonium methacrylate copolymer (RLPO)/dimethylaminoethyl methacrylate copolymer (EPO), polyvinylpyrroline (PVP)/polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus) and perphenazine (PPZ)...
March 22, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28342749/characterizing-the-differential-roles-of-striatal-5-ht1a-auto-and-hetero-receptors-in-the-reduction-of-l-dopa-induced-dyskinesia
#11
Samantha M Meadows, Nicole Chambers, Melissa M Conti, Sharon C Bossert, Crystal Tasber, Eitan Sheena, Mark Varney, Adrian Newman-Tancredi, Christopher Bishop
l-DOPA remains the benchmark treatment for Parkinson's disease (PD) motor symptoms, but chronic use leads to l-DOPA-induced dyskinesia (LID). The serotonin (5-HT) system has been established as a key modulator of LID and 5-HT1A receptors (5-HT1AR) stimulation has been shown to convey anti-dyskinetic effects. However, 5-HT1AR agonists often compromise clinical efficacy or display intrinsic side effects and their site(s) of actions remain debatable. Recently, highly selective G-protein biased 5-HT1AR agonists, F13714 and F15599, were shown to potently target 5-HT1A auto- or hetero-receptors, respectively...
March 22, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28342721/four-year-follow-up-of-the-changes-in-anterior-segment-after-phakic-collamer-lens-icl-implantation
#12
Yuanyuan Lu, Na Yang, Xuedong Li, Jun Kong
PURPOSE: To assess the changes and relationship in central vaulting, flare intensity and crystalline lens thickness during a follow-up period of 4 years after Implantable Collamer Lens (ICL) implantation in eyes with high myopia. DESIGN: Retrospective observational study. METHODS: 98 eyes of 50 patients were followed up with routine measurements of central vaulting, crystalline lens thickness, endothelial cell density and aqueous flare postoperatively...
March 22, 2017: American Journal of Ophthalmology
https://www.readbyqxmd.com/read/28342403/fitting-mas-nmr-spectra-in-crystals-with-local-disorder-czjzek-s-vs-maurer-s-model-for-11-b-and-71-ga-in-polycrystalline-gallium-borate
#13
K Seleznyova, N A Sergeev, M Olszewski, P Stępień, S V Yagupov, M B Strugatsky, J Kliava
A comparative analysis of the Czjzek's and Maurer's models of the joint distribution density of NMR quadrupole parameters has been carried out in view of their application to account for spectra broadening induced by local disorder in crystals. As an example of such an application, we have considered Magic Angle Spinning NMR of (11)B and (71)Ga isotopes in polycrystalline gallium borate. Computer simulations carried out using both models unambiguously show that in the case of low local disorder the Maurer's model, in contrast to the Czjzek's model, provides satisfactory fits to experimental NMR spectra...
March 18, 2017: Solid State Nuclear Magnetic Resonance
https://www.readbyqxmd.com/read/28342311/lengthy-one-dimensional-magnetite-fe3o4-sub-microfibers-with-excellent-electrochemical-performance
#14
Jianchao Ma, Jiali Chang, Hongzhu Ma, Duoduo Zhang, Qingliang Ma, Shaobin Wang
One dimensional Fe3O4 sub-microfibers with an average diameter of about 920nm and length of about 25μm were prepared by hydrothermal synthesis in the presence of sodium citrate (Na3cit). The physicochemical properties were characterized by X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). It was found that Fe3O4 crystal nuclei were generated from different Fe(2+)-citrate complexes under hydrothermal conditions and Na3cit as a capping agent promoted the formation of Fe3O4 microfibers...
March 18, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28340412/discovery-of-2-substituted-1h-benzo-d-immidazole-4-carboxamide-derivatives-as-novel-poly-adp-ribose-polymerase-1-inhibitors-with-in%C3%A2-vivo-anti-tumor-activity
#15
Jie Zhou, Ming Ji, Zhixiang Zhu, Ran Cao, Xiaoguang Chen, Bailing Xu
Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1 cells (PF50 = 7...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340400/pharmacoinformatics-exploration-of-polyphenol-oxidases-leading-to-novel-inhibitors-by-virtual-screening-and-molecular-dynamic-simulation-study
#16
Mubashir Hassan, Qamar Abbas, Zaman Ashraf, Ahmed A Moustafa, Sung-Yum Seo
Polyphenol oxidases (PPOs)/tyrosinases are metal-dependent enzymes and known as important targets for melanogenesis. Although considerable attempts have been conducted to control the melanin-associated diseases by using various inhibitors. However, the exploration of the best anti-melanin inhibitor without side effect still remains a challenge in drug discovery. In present study, protein structure prediction, ligand-based pharmacophore modeling, virtual screening, molecular docking and dynamic simulation study were used to screen the strong novel inhibitor to cure melanogenesis...
March 15, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28340391/optimization-of-the-marinelli-beaker-dimensions-using-genetic-algorithm
#17
Seyed Mehrdad Zamzamian, Seyed Abolfazl Hosseini, Mohammad Samadfam
A computational code, based on the genetic algorithm and MCNPX version 2.6 code was developed and used to investigate the effects of some important parameters of HPGe detector (such as Al cap thickness, dead-layer thickness and Ge hole size) on optimum dimensions of marinelli beaker. In addition, the effects of detector material on optimal beaker dimensions were also investigated. Finally, the optimized beaker dimensions at various beaker volumes (300, 500, 700, 1000 and 1500 cm(3)) were determined for some conventional Ge detectors with different crystal sizes (16 sizes)...
March 21, 2017: Journal of Environmental Radioactivity
https://www.readbyqxmd.com/read/28340368/synthesis-molecular-docking-antimycobacterial-and-antimicrobial-evaluation-of-new-pyrrolo-3-2-c-pyridine-mannich-bases
#18
Gilish Jose, Tholappanavara H Suresha Kumara, Haliwana B V Sowmya, Dharmarajan Sriram, Tayur N Guru Row, Amar A Hosamani, Sunil S More, Bhavya Janardhan, B G Harish, Sandeep Telkar, Yalegara Siddappa Ravikumar
In this report, we describe the synthesis and biological evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases (7a-v). The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold (6a-c) with secondary amines and excess of formaldehyde solution in AcOH. The chemical structures of the compounds were characterized by (1)H NMR, (13)C NMR, LC/MS and elemental analysis. Single crystal X-ray diffraction has been recorded for compound 7k ([C23H29ClN4](+2), H2O)...
March 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340354/mechanism-of-substrate-translocation-in-an-alternating-access-transporter
#19
Naomi R Latorraca, Nathan M Fastman, A J Venkatakrishnan, Wolf B Frommer, Ron O Dror, Liang Feng
Transporters shuttle molecules across cell membranes by alternating among distinct conformational states. Fundamental questions remain about how transporters transition between states and how such structural rearrangements regulate substrate translocation. Here, we capture the translocation process by crystallography and unguided molecular dynamics simulations, providing an atomic-level description of alternating access transport. Simulations of a SWEET-family transporter initiated from an outward-open, glucose-bound structure reported here spontaneously adopt occluded and inward-open conformations...
March 23, 2017: Cell
https://www.readbyqxmd.com/read/28340294/a-well-defined-osmium-cupin-complex-hyperstable-artificial-osmium-peroxygenase
#20
Nobutaka Fujieda, Takumi Nakano, Yuki Taniguchi, Haruna Ichihashi, Hideki Sugimoto, Yuma Morimoto, Yosuke Nishikawa, Genji Kurisu, Shinobu Itoh
Thermally stable TM1459 cupin superfamily protein from Thermotoga maritima was repurposed as an osmium (Os) peroxygenase by metal-substitution strategy employing the metal-binding promiscuity. This novel artificial metalloenzyme bears a datively bound Os ion supported by the 4-histidine motif. The well-defined Os center is responsible for not only the catalytic activity but also the thermodynamic stability of the protein folding, leading to the robust biocatalyst (Tm ≈ 120 °C). The spectroscopic analysis and atomic resolution X-ray crystal structures of Os-bound TM1459 revealed two types of donor sets to Os center with octahedral coordination geometry...
March 24, 2017: Journal of the American Chemical Society
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