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https://www.readbyqxmd.com/read/28432987/multimodal-imaging-of-language-reorganization-in-patients-with-left-temporal-lobe-epilepsy
#1
Yu-Hsuan A Chang, Nobuko Kemmotsu, Kelly M Leyden, N Erkut Kucukboyaci, Vicente J Iragui, Evelyn S Tecoma, Leena Kansal, Marc A Norman, Rachelle Compton, Tobin J Ehrlich, Vedang S Uttarwar, Anny Reyes, Brianna M Paul, Carrie R McDonald
This study explored the relationships among multimodal imaging, clinical features, and language impairment in patients with left temporal lobe epilepsy (LTLE). Fourteen patients with LTLE and 26 controls underwent structural MRI, functional MRI, diffusion tensor imaging, and neuropsychological language tasks. Laterality indices were calculated for each imaging modality and a principal component (PC) was derived from language measures. Correlations were performed among imaging measures, as well as to the language PC...
April 19, 2017: Brain and Language
https://www.readbyqxmd.com/read/28432725/synthesis-and-biological-potency-of-anilino-triazine-insecticides
#2
Timothy C Johnson, Annette V Brown, Kristy K Bryan, Katherine K Guenthenspberger, Ricky Hunter, Timothy P Martin, Noormohamed Niyaz, Gene F Tisdell, Tony Trullinger
BACKGROUND: An insecticide screening effort identified N-(4-bromophenyl)-4,6-bis(2,2,2-trifluoroethoxy)-1,3,5-triazine-2-amine as having weak potency against two Lepidopteran species, Helicoverpa zea and Spodoptera exigua. A structure activity relationship study about the trifluoroethoxy substituents and the aniline of this compound was carried out in an effort to improve insecticidal potency. RESULTS: Initially, a series of analogs bearing various substituents on the aniline were prepared and the insecticidal potency was evaluated against Helicoverpa zea and Spodoptera exigua in greenhouse diet feeding assays...
April 22, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28432448/resistance-to-radial-expansion-limits-muscle-strain-and-work
#3
E Azizi, A R Deslauriers, N C Holt, C E Eaton
The collagenous extracellular matrix (ECM) of skeletal muscle functions to transmit force, protect sensitive structures, and generate passive tension to resist stretch. The mechanical properties of the ECM change with age, atrophy, and neuromuscular pathologies, resulting in an increase in the relative amount of collagen and an increase in stiffness. Although numerous studies have focused on the effect of muscle fibrosis on passive muscle stiffness, few have examined how these structural changes may compromise contractile performance...
April 21, 2017: Biomechanics and Modeling in Mechanobiology
https://www.readbyqxmd.com/read/28432424/variations-of-isovaline-structure-related-to-activity-in-the-formalin-foot-assay-in-mice
#4
Timothy Fung, Yahya I Asiri, Richard Wall, Stephan K W Schwarz, Ernest Puil, Bernard A MacLeod
Current centrally acting analgesics such as opioids are associated with adverse effects that limit their use and threaten patient safety. Isovaline is a novel prototype analgesic that produces peripheral antinociception in several pain models with little or no effect on the central nervous system. The aim of this study was to establish a preliminary structure-activity relationship for isovaline derivatives by assaying efficacy in the formalin foot assay and central adverse effect profile in mice. Selected compounds were tested using the formalin foot assay to determine efficacy in reducing formalin-induced behaviors...
April 21, 2017: Amino Acids
https://www.readbyqxmd.com/read/28432142/structural-similarities-between-neuregulin-1-3-isoforms-determine-their-subcellular-distribution-and-signaling-mode-in-central-neurons
#5
Detlef Vullhorst, Tanveer Ahmad, Irina Karavanova, Carolyn Keating, Andres Buonanno
The Neuregulin (NRG) family of ErbB ligands is comprised of numerous variants originating from the use of different genes, alternative promoters and splice variants. NRGs have generally been thought to be transported to axons and presynaptic terminals where they signal via ErbB3/4 receptors in paracrine or juxtacrine mode. However, we recently demonstrated that unprocessed pro-NRG2 accumulates on cell bodies and proximal dendrites, and that NMDAR activity is required for shedding of its ectodomain by metalloproteinases...
April 21, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28431978/temporal-niche-switching-in-arabian-oryx-oryx-leucoryx-seasonal-plasticity-of-24h-activity-patterns-in-a-large-desert-mammal
#6
Joshua G Davimes, Abdulaziz N Alagaili, Mads F Bertelsen, Osama B Mohammed, Jason Hemingway, Nigel C Bennett, Paul R Manger, Nadine Gravett
The Arabian oryx, a moderately large mammal that inhabits a harsh desert environment, has been shown to exhibit seasonal variations in activity and inactivity patterns. Here we analyzed the continuous year-round activity patterns of twelve free-roaming Arabian oryx under natural conditions from two varying desert environments in Saudi Arabia using abdominally implanted activity meters. We simultaneously recorded weather parameters at both sites to determine whether environmental factors are responsible for temporal niche switching as well as the seasonal structuring and timing of this behavioural plasticity...
April 18, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28431352/degradation-of-sulfamethoxazole-by-uv-uv-h2o2-and-uv-persulfate-pds-formation-of-oxidation-products-and-effect-of-bicarbonate
#7
Yi Yang, Xinglin Lu, Jin Jiang, Jun Ma, Guanqi Liu, Ying Cao, Weili Liu, Juan Li, Suyan Pang, Xiujuan Kong, Congwei Luo
The frequent detection of sulfamethoxazole (SMX) in wastewater and surface waters gives rise of concerns about their ecotoxicological effects and potential risks to induce antibacterial resistant genes. UV/hydrogen peroxide (UV/H2O2) and UV/persulfate (UV/PDS) advanced oxidation processes have been demonstrated to be effective for the elimination of SMX, but there is still a need for a deeper understanding of product formations. In this study, we identified and compared the transformation products of SMX in UV, UV/H2O2 and UV/PDS processes...
March 28, 2017: Water Research
https://www.readbyqxmd.com/read/28431348/evaluation-of-structural-effects-on-the-flocculation-performance-of-a-co-graft-starch-based-flocculant
#8
Zhouzhou Liu, Hua Wei, Aimin Li, Hu Yang
The molecular structure of a material substantially determines its final application performance. In this work, a series of starch-based flocculants with different charge densities and average graft chain lengths were prepared by the co-graft polymerization of acrylamide and [(2-methacryloyloxyethyl) trimethyl ammonium chloride] (St-g-PAM-co-PDMC). The flocculation performance of St-g-PAM-co-PDMC was studied systematically at neutral pH using kaolin suspension and sodium humate (NaHA) aqueous solution as synthetic wastewaters...
April 18, 2017: Water Research
https://www.readbyqxmd.com/read/28431342/discovery-of-tetrahydrocarbazoles-as-dual-perk-and-prb-inhibitors
#9
Mahesh R Kulkarni, Madhav S Mane, Usha Ghosh, Rajiv Sharma, Nitin P Lad, Ankita Srivastava, Asha Kulkarni-Almeida, Prashant S Kharkar, Vijay M Khedkar, Shivaji S Pandit
The extracellular signal-regulated kinase (ERK) is one of the most important molecular targets for cancer that controls diverse cellular processes such as proliferation, survival, differentiation and motility. Similarly, the Rb (retinoblastoma protein) is a tumor suppressor protein and its function is to prevent excessive cell growth by inhibiting cell cycle progression. When the cell is ready to divide, pRb is phosphorylated, becomes inactive and allows cell cycle progression. Herein, we discovered a new series of tetrahydrocarbazoles as dual inhibitors of pERK and pRb phosphorylation...
March 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431339/novel-coumarin-and-quinolinone-based-polycycles-as-cell-division-cycle-25-a-and-c-phosphatases-inhibitors-induce-proliferation-arrest-and-apoptosis-in-cancer-cells
#10
Clemens Zwergel, Brigitte Czepukojc, Emilie Evain-Bana, Zhanjie Xu, Giulia Stazi, Mattia Mori, Alexandros Patsilinakos, Antonello Mai, Bruno Botta, Rino Ragno, Denise Bagrel, Gilbert Kirsch, Peter Meiser, Claus Jacob, Mathias Montenarh, Sergio Valente
Cell division cycle phosphatases CDC25 A, B and C are involved in modulating cell cycle processes and are found overexpressed in a large panel of cancer typology. Here, we describe the development of two novel quinone-polycycle series of CDC25A and C inhibitors on the one hand 1a-k, coumarin-based, and on the other 2a-g, quinolinone-based, which inhibit either enzymes up to a sub-micro molar level and at single-digit micro molar concentrations, respectively. When tested in six different cancer cell lines, compound 2c displayed the highest efficacy to arrest cell viability, showing in almost all cell lines sub-micro molar IC50 values, a profile even better than the reference compound NCS95397...
April 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28430099/mutual-interaction-enables-the-mycobacterial-plasmid-pal5000-origin-binding-protein-repb-to-recruit-repa-the-plasmid-replicase-to-the-origin
#11
Soniya Chatterjee, Madhu Manti Patra, Sourabh Samaddar, Arnab Basu, Sujoy K Das Gupta
The Mycobacterium fortuitum plasmid, pAL5000, is the most-studied member of a family of plasmids that are found in Actinobacteria. Its replication is brought about by the combined action of two plasmid-encoded replication proteins, RepA and RepB. RepB has earlier been shown to be a sigma factor homologue that possesses origin-binding activity. The mechanism by which RepA functions, and its relationship with RepB, if any, has not been explored yet. In this study, we show that RepA shares a common catalytic domain, with proteins belonging to the primase-polymerase and DNA polymerase X families...
April 22, 2017: Microbiology
https://www.readbyqxmd.com/read/28428543/microspectrofluorimetry-to-dissect-the-permeation-of-ceftazidime-in-gram-negative-bacteria
#12
Anas Allam, Laure Maigre, Julia Vergalli, Estelle Dumont, Bertrand Cinquin, Rodolphe Alves de Sousa, Jelena Pajovic, Elizabeth Pinet, Nikaia Smith, Jean-Philippe Herbeuval, Matthieu Réfrégiers, Isabelle Artaud, Jean-Marie Pagès
A main challenge in chemotherapy is to determine the in cellulo parameters modulating the drug concentration required for therapeutic action. It is absolutely urgent to understand membrane permeation and intracellular concentration of antibiotics in clinical isolates: passing the membrane barrier to reach the threshold concentration inside the bacterial periplasm or cytoplasm is the pivotal step of antibacterial activity. Ceftazidime (CAZ) is a key molecule of the combination therapy for treating resistant bacteria...
April 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28428085/galloylation-of-polyphenols-alters-their-biological-activity
#13
REVIEW
Daniel Karas, Jitka Ulrichová, Kateřina Valentová
Polyphenols form one of the largest groups of natural compounds and possess a wide range of biological properties. These activities can be influenced by the galloyl moiety within their structures. A multitude of galloylated polyphenolic compounds occurs in nature, but galloylated phenols are also produced synthetically to influence their biological properties. This review provides a comprehensive summary of current knowledge about natural (galloylated catechins, theaflavins and proanthocyanidins, penta-O-galloyl-β-D-glucose, gallotannins, ellagitannins, ellagic acid and flavonols) and semisynthetic gallates with a focus on their biological activity and toxicity issues...
April 17, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28428042/synthesis-and-biological-evaluation-of-selective-tubulin-inhibitors-as-anti-trypanosomal-agents
#14
Viharika Bobba, Vishal Nanavaty, Nethrie D Idippily, Anran Zhao, Bibo Li, Bin Su
African trypanosomiasis is still a threat to human health due to the severe side-effects of current drugs. We identified selective tubulin inhibitors that showed the promise to the treatment of this disease, which was based on the tubulin protein structural difference between mammalian and trypanosome cells. Further lead optimization was performed in the current study to improve the efficiency of the drug candidates. We used Trypanosoma brucei brucei cells as the parasite model, and human normal kidney cells and mouse macrophage cells as the host model to evaluate the compounds...
April 8, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28428040/design-synthesis-and-docking-studies-of-quinazoline-analogues-bearing-aryl-semicarbazone-scaffolds-as-potent-egfr-inhibitors
#15
Yuanbiao Tu, Caolin Wang, Shan Xu, Zhou Lan, Wei Li, Jiaqian Han, Yuanzhang Zhou, Pengwu Zheng, Wufu Zhu
Two series of quinazoline derivatives bearing aryl semicarbazone scaffolds (9a-o and 10a-o) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7 and PC-3). The selected compound 9o was further evaluated for the inhibitory activity against EGFR kinases. Four of the compounds showed excellent cytotoxicity activity and selectivity with the IC50 values in single-digit μM to nanomole range. Two of them are equal to more active than positive control afatinib against one or more cell lines...
April 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28427850/five-year-changes-in-cardiac-structure-and-function-in-patients-with-rheumatoid-arthritis-compared-with-the-general-population
#16
John M Davis, Grace Lin, Jae K Oh, Cynthia S Crowson, Sara J Achenbach, Terry M Therneau, Eric L Matteson, Richard J Rodeheffer, Sherine E Gabriel
BACKGROUND: Patients with rheumatoid arthritis (RA) have increased risk of heart failure with preserved ejection fraction. The development and progression of left ventricular dysfunction before onset of clinical heart failure are unknown. The objective of this study was to evaluate longitudinal changes in cardiac structure and function of patients with RA compared with persons in the general population. METHODS: A prospective longitudinal study of a population-based cohort of 160 patients with RA and a population-based cohort of 1391 persons without RA (non-RA cohort) was performed...
March 31, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28427812/synthesis-and-evaluation-of-4-6-disubstituted-pyrimidines-as-cns-penetrant-pan-muscarinic-antagonists-with-a-novel-chemotype
#17
Aaron M Bender, Rebecca L Weiner, Vincent B Luscombe, Hyekyung P Cho, Colleen M Niswender, Darren W Engers, Thomas M Bridges, P Jeffrey Conn, Craig W Lindsley
This letter describes the synthesis and structure activity relationship (SAR) studies of structurally novel M4 antagonists, based on a 4,6-disubstituted core, identified from a high-throughput screening campaign. A multi-dimensional optimization effort enhanced potency at both human and rat M4 (IC50s<300nM), with no substantial species differences noted. Moreover, CNS penetration proved attractive for this series (brain:plasma Kp,uu=0.87), while other DMPK attributes were addressed in the course of the optimization effort, providing low in vivo clearance in rat (CLp=5...
April 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28427811/new-derivatives-of-ursolic-acid-through-the-biotransformation-by-bacillus-megaterium-cgmcc-1-1741-as-inhibitors-on-nitric-oxide-production
#18
Chao Zhang, Shao-Hua Xu, Bai-Ling Ma, Wei-Wei Wang, Bo-Yang Yu, Jian Zhang
Microbial transformation of ursolic acid (1) by Bacillus megaterium CGMCC 1.1741 was investigated and yielded five metabolites identified as 3-oxo-urs-12-en-28-oic acid (2); 1β,11α-dihydroxy-3-oxo-urs-12-en-28-oic acid (3); 1β-hydroxy-3-oxo-urs-12-en-28, 13-lactoe (4); 1β,3β, 11α-trihydroxyurs-12-en-28-oic acid (5) and 1β,11α-dihydroxy-3-oxo-urs-12-en-28-O-β-d-glucopyranoside (6). Metabolites 3, 4, 5 and 6 were new natural products. Their nitric oxide (NO) production inhibitory activity was assessed in lipopolysaccharide (LPS) - stimulated RAW 264...
March 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28427810/synthesis-of-novel-5-6-dehydrokawain-analogs-as-osteogenic-inducers-and-their-action-mechanisms
#19
Momochika Kumagai, Keisuke Nishikawa, Takashi Mishima, Izumi Yoshida, Masahiro Ide, Keiko Koizumi, Munetomo Nakamura, Yoshiki Morimoto
An imbalance between bone resorption by osteoclasts and bone formation by osteoblasts can cause bone loss and bone-related disease. In a previous search for natural products that increase osteogenic activity, we found that 5,6-dehydrokawain (1) from Alpinia zerumbet promotes osteoblastogenesis. In this study, we synthesized and evaluated series of 5,6-dehydrokawain analogs. Our structure-activity relationships revealed that alkylation of para or meta position of aromatic ring of 1 promote osteogenic activity...
April 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28427558/a-computational-approach-to-identify-the-biophysical-and-structural-aspects-of-methylenetetrahydrofolate-reductase-mthfr-mutations-a222v-e429a-and-r594q-leading-to-schizophrenia
#20
Himani Tanwar, P Sneha, D Thirumal Kumar, R Siva, Charles Emmanuel Jebaraj Walter, C George Priya Doss
The association between depression and methylenetetrahydrofolate reductase (MTHFR) has been continually demonstrated in clinical studies, yet there are sparse resources available to build a relationship between the mutations associated with MTHFR and depression. The common mutations found to be associated with schizophrenia and MTHFR are A222V, E429A, and R594Q. Although abundant research on structural and functional effects caused by A222V mutation is available, very less amount of studies have been done on the other two mutants (E429A and R594Q)...
2017: Advances in Protein Chemistry and Structural Biology
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