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https://www.readbyqxmd.com/read/28636281/aryl-and-heteroaryl-substituted-phenylalanines-as-ampa-receptor-ligands
#1
Ewa Szymańska, Paulina Chałupnik, Tommy N Johansen, Birgitte Nielsen, Ana Maria Cuñado Moral, Darryl S Pickering, Anna Więckowska, Katarzyna Kieć-Kononowicz
A series of racemic unnatural amino acids was rationally designed on the basis of recently published X-ray structures of the GluA2 LBD with bound phenylalanine-based antagonists. Twelve new diaryl- or aryl/heteroaryl-substituted phenylalanine derivatives were synthesized and evaluated in vitro in radioligand binding assays at native rat ionotropic glutamate receptors. The most interesting compound in this series, (RS)-2-amino-3-(3'-hydroxy-5-(1H-pyrazol-4-yl)-[1,1'-biphenyl]-3-yl)propanoic acid 7e, showed the binding affinity of 4...
June 21, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28636268/high-throughput-sequencing-reveals-drosophila-suzukii-responses-to-insecticides
#2
Ruchir Mishra, Joanna C Chiu, Gang Hua, Nilesh R Tawari, Michael J Adang, Ashfaq A Sial
Global climate change and acquired resistance to insecticides are threats to world food security. Drosophila suzukii, a devastating invasive pest in many parts of the world, causes substantial economic losses to fruit production industries, forcing farmers to apply broad-spectrum insecticides frequently. This could lead to the development of insecticide resistance. We determined the Lethal Concentration50 (median lethal concentration) values of zeta-cypermethrin, spinosad, and malathion insecticides against D...
June 21, 2017: Insect Science
https://www.readbyqxmd.com/read/28636252/influence-of-analyzed-lubricant-volumes-on-the-amount-and-characteristics-of-generated-wear-particles-from-three-different-types-of-polyethylene-liner-materials
#3
Jana Markhoff, Carmen Zietz, Christian Fabry, Gerhard Fulda, Rainer Bader
The articulating components of artificial joints consist mainly of metals, ceramics, or polymers. Resulting abrasive wear particles can promote osteolysis and aseptic loosening of the endo-prosthetic implants. Ultra-high-molecular-weight-polyethylene is the material used most for bearing couples in total hip replacement. In the present study, three types of polyethylene (PE) liners varying in material composition, i.e., (1) conventional PE (C-PE), (2) sequentially cross-linked PE (SX-PE), (3) cross-linked PE blended with vitamin E (EX-PE) articulating with two types of femoral heads were used...
June 21, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/28636217/research-on-potential-biomarker-correlates-for-suicidal-behavior-a-review
#4
REVIEW
Sangha Kim, Kyoung-Uk Lee
Suicide is a world health priority. Studies over the last few decades have revealed the complexity underlying the neurobiological mechanisms of suicide. Researchers have found dysregulations in the serotonergic system, the stress system, neural plasticity, lipid metabolism, and cell signaling pathways in relation to suicidal behaviors. These findings have provided more insight into the final path leading to suicide, at which medical intervention should be applied to prevent the action. However, because these molecular mechanisms have been implicated in both depression and suicide, the specificity of the mechanisms has been obscured...
June 21, 2017: Asia-Pacific Psychiatry: Official Journal of the Pacific Rim College of Psychiatrists
https://www.readbyqxmd.com/read/28636199/widespread-occurrence-and-potential-for-biodegradation-of-bioactive-contaminants-in-congaree-national-park-usa
#5
Paul M Bradley, William A Battaglin, Jimmy M Clark, Frank Henning, Michelle L Hladik, Luke R Iwanowicz, Celeste A Journey, Jeffrey W Riley, Kristin M Romanok
Organic contaminants with designed molecular bioactivity, such as pesticides and pharmaceuticals, originate from human and agricultural sources, occur frequently in surface waters, and threaten the structure and function of aquatic and terrestrial ecosystems. Congaree National Park in South Carolina (USA) is a vulnerable park unit due to its location downstream of multiple urban and agricultural contaminant sources and its hydrologic setting, being composed almost entirely of floodplain and aquatic environments...
June 21, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28636190/uchl1-promotes-invasion-of-breast-cancer-cells-through-activating-akt-signaling-pathway
#6
Yanhong Luo, Jianfeng He, Chunlin Yang, Matthew Orange, Xingcong Ren, Nick Blair, Tao Tan, Jin-Ming Yang, Hua Zhu
As a de-ubiquitin enzyme, ubiquitin C-terminal hydrolase (UCH)-L1 has been shown to be overexpressed in several human cancers. However, the function of UCH-L1 in invasion of breast cancers is still unclear. Here we report that the expression of UCH-L1 is significantly higher in cancer cells with higher invasive ability. While ectopic UCH-L1 expression failed to alter cell proliferation in MCF-7 cells, it caused a significant upregulation of cellular invasion. Furthermore, siRNA mediated knockdown of UCH-L1 led to suppression of invasion in UCH-L1 overexpressing MCF-7 cells...
June 21, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28636189/discovery-of-alkyl-bis-oxy-dibenzimidamide-derivatives-as-novel-protein-arginine-methyltransferase-1-prmt1-inhibitors
#7
Wei-Yao Zhang, Wen-Chao Lu, Hao Jiang, Zheng-Bing Lv, Yi-Qian Xie, Fu-Lin Lian, Zhong-Jie Liang, Yu-Xi Jiang, Da-Jin Wang, Cheng Luo, Jia Jin, Fei Ye
Protein arginine methylation, a post-translational modification critical for a variety of biological processes, is catalyzed by protein arginine N-methyltransferases (PRMTs). In particular, PRMT1 is responsible for over 85% of the arginine methylation in mammalian cells. Dysregulation of PRMT1 is involved in diverse pathological diseases including cancers. However, most current PRMT1inhibitors are lack of specificity, efficacy, and bioavailability. Herein, a series of alkyl bis(oxy)dibenzimidamide derivatives were identified as selective PRMT1 inhibitors...
June 21, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28636181/identification-of-biomarkers-for-early-diagnosis-of-acute-myocardial-infarction
#8
Wen-Han Ge, Yong Lin, Sen Li, Xuefeng Zong, Zhong-Chun Ge
Acute myocardial infarction (AMI) is a common disease with serious consequences in mortality and cost. Here we aim to screen the differentially expressed genes (DEGs) as biomarkers for early diagnosis of AMI. The microarray data of AMI was downloaded from Gene Expression Omnibus (GEO), including two independent types of research GSE66360 and GSE62646. The DEGs between control and processed samples were screened out by using limma package. Meanwhile, we performed functional analysis of GO terms and/or KEGG pathways to observe the enriched pathways of the DEGs...
June 21, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28636162/cobalt-catalyzed-ortho-c-h-functionalization-alkyne-annulation-of-benzylamine-derivatives-access-to-dihydroisoquinolines
#9
Angel Manu Martínez, Nuria Rodríguez, Ramon Gomez-Arrayas, Juan C Carretero
A practical picolinamide-directed C-H functionalization/alkyne annulation of benzylamine derivatives enabling the access to the previously elusive 1,4-dihydroisoquinoline skeleton was developed using molecular O2 as the sole oxidant and Co(OAc)2 as precatalyst. The method is compatible with both internal and terminal alkynes and shows high versatility and functional-group tolerance. Furthermore, full preservation of enantiopurity is observed when using non-racemic alpha-substituted benzylamine derivatives...
June 21, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28636152/dynamics-and-origin-of-cytokinins-involved-in-plant-manipulation-by-a-leaf-mining-insect
#10
Hui Zhang, Antoine Guiguet, Géraldine Dubreuil, Anna Kisiala, Peter Andreas, R J Neil Emery, Elisabeth Huguet, Mélanie Body, David Giron
Several herbivorous insects and plant-associated microorganisms control the phytohormonal balance, thus enabling them to successfully exploit the plant by inhibiting plant defences and withdrawing plant resources for their own benefit. The leaf-mining moth Phyllonorycter blancardella modifies the cytokinin (CK) profile of mined leaf-tissues, and the insect symbiotic bacteria Wolbachia is involved in the plant manipulation to the benefit of the insect host. To gain a deeper understanding into the possible origin and dynamics of CKs, we conducted an extensive characterization of CKs in larvae and in infected apple leaves...
June 21, 2017: Insect Science
https://www.readbyqxmd.com/read/28636114/set-i2pp2a-overexpression-induces-phenotypic-molecular-and-metabolic-alterations-in-an-oral-keratinocyte-cell-line
#11
Lays M Sobral, Ricardo D Coletta, Luciane C Alberici, Carlos Curti, Andréia Machado Leopoldino
The multifunctional SET/I2PP2A protein is known to be overexpressed in head and neck squamous cell carcinoma. However, SET has been reported to have apparently conflicting roles in promoting cancer cell survival under oxidative stress conditions and preventing invasion and metastasis, complicating efforts to understand the contribution of SET to carcinogenesis. In the present study, we overexpressed SET in a spontaneously immortalized oral keratinocyte cell line (NOK-SI SET) and demonstrated that SET up-regulation alone was sufficient to transform cells...
June 21, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28636075/molecular-cloning-mrna-expression-and-biological-activity-of-the-pheromone-biosynthesis-activating-neuropeptide-pban-from-the-european-corn-borer-ostrinia-nubilalis
#12
J Fodor, G Köblös, Á Kákai, Z Kárpáti, B P Molnár, T Dankó, G Bozsik, C Bognár, G Szőcs, A Fónagy
Pheromone biosynthesis activating neuropeptide (PBAN) is a member of the pyrokinin (FXPRLamide) insect neuropeptides. Here, we report the cloning of the gene Ostnu-PBAN from the E and Z pheromone strains of the European corn borer (ECB), Ostrinia nubilalis (Lepidoptera: Crambidae), a major pest of maize. The Ostnu-PBAN genomic sequence is > 5 kb in length and consists of six exons. The deduced amino acid sequence revealed a 200-residue precursor protein including a signal peptide, a 24-amino acid (aa) diapause hormone, a 37-aa PBAN and three other FXPRLamide neuropeptides...
June 21, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28636053/evidence-of-bad-recycling-practices-bfrs-in-children-s-toys-and-food-contact-articles
#13
A Guzzonato, F Puype, S J Harrad
Brominated flame retardants (BFRs) have been used intentionally in a wide range of plastics, but are now found in an even wider range of such materials (including children's toys and food contact articles) as a result of recycling practices that mix BFR-containing waste plastics with "virgin" materials. In this study Br was quantified in toy and food contact samples on the assumption that its concentration can be used as a metric for BFR contamination. Subsequently, compound specific determination of BFRs was performed to evaluate the validity of the aforementioned assumption, crucial to render rapid, inexpensive, in situ Br determination in non-laboratory environments (such as waste handling facilities) a viable option for sorting wastes according to their BFR content...
June 21, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28636032/reline-aqueous-solutions-behaving-as-liquid-mixtures-of-h-bonded-co-solvents-microphase-segregation-and-formation-of-co-continuous-structures-as-indicated-by-brillouin-and-1-h-nmr-spectroscopies
#14
E Posada, N López-Salas, R J Jiménez Riobóo, M L Ferrer, M C Gutiérrez, F Del Monte
Deep eutectic solvents (DESs) offer a suitable alternative to conventional solvents in terms of both performance and cost-effectiveness. Some DESs also offer certain green features, the greenness of which is notoriously enhanced when combined with water. Aqueous DES dilutions are therefore attracting great attention as a novel green medium for biotechnological processes, with the aqueous dilutions of reline - a DES composed of urea and choline chloride - being one of the most studied systems. Despite their macroscopic homogeneous appearance, both (1)H NMR spectroscopic studies and molecular dynamics simulations have revealed the occurrence of certain dynamic heterogeneity at a microscopic molecular level...
June 21, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28636028/supramolecular-functional-assemblies-dynamic-membrane-transporters-and-peptide-nanotubular-composites
#15
Alberto Fuertes, Marisa Juanes, Juan R Granja, Javier Montenegro
The fabrication of functional molecular devices constitutes one of the most important current challenges for chemical sciences. The complex processes accomplished by living systems continuously demand the assistance of non-covalent interactions between molecular building blocks. Additionally, these building blocks (proteins, membranes, nucleotides) are also constituted by self-assembled structures. Therefore, supramolecular chemistry is the discipline required to understand the properties of the minimal self-assembled building blocks of living systems and to develop new functional smart materials...
June 21, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28636001/wataa-atlas-of-protein-hydration-exploring-synergies-between-data-mining-and-ab-initio-calculations
#16
Jiří Černý, Bohdan Schneider, Lada Biedermannová
Water molecules represent an integral part of proteins and a key determinant of protein structure, dynamics and function. WatAA is a newly developed, web-based atlas of amino-acid hydration in proteins. The atlas provides information about the ordered first hydration shell of the most populated amino-acid conformers in proteins. The data presented in the atlas are drawn from two sources: experimental data and ab initio quantum-mechanics calculations. The experimental part is based on a data-mining study of a large set of high-resolution protein crystal structures...
June 21, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28635994/oral-field-cancerization-history-and-future-perspectives
#17
A Gabusi, L Morandi, S Asioli, M P Foschini
Notwithstanding extended surgical approaches or adjuvant chemoradiotherapy, the development of multiple neoplastic lesions arising in the oral cavity after treatment still represents a critical clinical challenge in the management of patients with oral squamous cell carcinoma. Such clinical behavior of oral squamous cell carcinoma is nowadays better known as "field" cancerization effect as suggested by Slaughter, the author that for the first time tried to describe it in a scientific paper. Field cancerization is now widely accepted not only in head and neck oncology but also in other anatomical districts as well as in different types of epithelial neoplasia...
March 2017: Pathologica
https://www.readbyqxmd.com/read/28635989/sinonasal-tumor-pathology-what-s-new
#18
A Franchi
The sinonasal tract is an anatomical region affected by a wide variety of tumors with different clinical behavior, histologic and molecular features. Substantial advances have been made in the field of sinonasal tumor pathology in recent years, including improvement in the diagnosis, treatment and genetic characterization. In this article, a review of the histological features of new distinctive pathologic entities as well as newly described molecular alterations of these rare tumors is presented.
March 2017: Pathologica
https://www.readbyqxmd.com/read/28635988/salivary-epithelial-myoepithelial-carcinoma-clinical-morphological-and-molecular-features
#19
R De Cecio, M Cantile, F Fulciniti, G Botti, M P Foschini, N S Losito
Epithelial-myoepithelial carcinoma (EMC) is a rare biphasic tumor accounting for less than 2% of all salivary gland malignancies. It presents as a slowly growing, asymptomatic small size mass, with ulceration of overlying mucosa in some cases. Microscopically, it is characterized by glands lined by the simultaneous presence of two different cell components, inner epithelial cells and outer myoepithelial cells. Immunohistochemical staining of myoepithelial cells is variably positive for vimentin, Smooth Muscle Actin (SMA), Muscle Specific Actin (MSA), S100, Smooth Muscle Myosin Heavy Chain I(SM-MHC), calponin and p63...
March 2017: Pathologica
https://www.readbyqxmd.com/read/28635962/growth-of-organic-crystals-via-attachment-and-transformation-of-nanoscopic-precursors
#20
Yuan Jiang, Matthias Kellermeier, Denis Gebaue, Zihao Lu, Rose Rosenberg, Adrian Moise, Michael Przybylski, Helmut Cölfen
A key requirement for the understanding of crystal growth is to detect how new layers form and grow at the nanoscale. Multistage crystallization pathways involving liquid-like, amorphous or metastable crystalline precursors have been predicted by theoretical work and have been observed experimentally. Nevertheless, there is no clear evidence that any of these precursors can also be relevant for the growth of crystals of organic compounds. Herein, we present a new growth mode for crystals of DL-glutamic acid monohydrate that proceeds through the attachment of preformed nanoscopic species from solution, their subsequent decrease in height at the surface and final transformation into crystalline 2D nuclei that eventually build new molecular layers by further monomer incorporation...
June 21, 2017: Nature Communications
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