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https://www.readbyqxmd.com/read/28445950/the-discovery-of-a-novel-compound-with-potent-antitumor-activity-virtual-screening-synthesis-biological-evaluation-and-preliminary-mechanism-study
#1
Yuanyuan Jin, Linhu Li, Zhaoyong Yang, Mingliang Liu, Huiyuan Guo, Weiyi Shen
Farnesyltransferase has been regarded as a promising drug target against cancer as it is critical for membrane association of several signal transduction proteins. In this study, a novel farnesyltransferase inhibitor (IMB-1406) was identified through virtual screening. It exhibits stronger potency (IC50s: 6.92-8.99 μM) than Sunitinib against all of the tested cancer cell lines. Preliminary studies on mechanism reveal that IMB-1406 induces apoptosis in HepG2 cells by arresting the cell cycle at the S phase, altering anti- and pro-apoptotic proteins leading to mitochondrial dysfunction and activation of caspase-3...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445828/targeting-the-aryl-hydrocarbon-receptor-nuclear-translocator-complex-with-dmog-and-stemregenin-1-improves-primitive-hematopoietic-stem-cell-expansion
#2
Carlo Stephan Jackson, Chrisna Durandt, Ilse Janse van Rensburg, Vincent Praloran, Philippe Brunet de la Grange, Michael Sean Pepper
Culture conditions used for the expansion of hematopoietic stem and progenitor cells (HSCs and HPCs, collectively HSPCs) should ideally favor the self renewal of long-term HSCs. At 20% O2, the synthesis of HIF-1α is balanced by its hydroxylation and proteasomal degradation. This favors HSPC differentiation, but can be prevented by culturing CD34+ cord blood cells in the presence of dimethyloxaloylglycine (DMOG). This differentiation may also be reduced by culturing the cells in the presence of Stemregenin 1, an antagonist of the aryl hydrocarbon receptor (AhR)...
April 20, 2017: Stem Cell Research
https://www.readbyqxmd.com/read/28445827/scale-effect-on-spatial-patterns-of-ecosystem-services-and-associations-among-them-in-semi-arid-area-a-case-study-in-ningxia-hui-autonomous-region-china
#3
Shuna Xu, Yanfang Liu, Xia Wang, Guangxia Zhang
Identifying scale effect on spatial patterns of ecosystem services and associations among them has been recognized as critical to the sustainable management of ecosystem services. We proposed a method to conveniently integrate ecosystem services of small scale into different larger scales. Taking Ningxia Hui Autonomous Region in west China as an example, we analyzed the change regularity of spatial patterns of 7 ecosystem services under 22 different scales. Further, the tradeoffs and synergies among ecosystem services across all scales were compared...
April 23, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28445820/the-synthesis-and-properties-of-linear-a-%C3%AF-d-%C3%AF-a-type-organic-small-molecule-containing-diketopyrrolopyrrole-terminal-units
#4
Shanshan Zhang, Qingfen Niu, Tao Sun, Yang Li, Tianduo Li, Haixia Liu
A novel linear A-π-D-π-A-type organic small molecule Ph2(PDPP)2 consisting diketopyrrolopyrrole (DPP) as acceptor unit, biphenylene as donor unit and acetylene unit as π-linkage has been successfully designed and synthesized. Its corresponding thermal, photophysical and electrochemical properties as well as the photoinduced charge-separation process were investigated. Ph2(PDPP)2 exhibits high thermal stability and it can be soluble in common organic solvents such as chloroform and tetrahydrofuran. The photophysical properties show that DPP2Ph2 harvests sunlight over the entire visible spectrum range in the thin-film state (300-800nm)...
April 20, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28445810/circulating-cadmium-concentration-and-risk-of-aortic-aneurysms-a-nested-case-control-study-within-the-malm%C3%A3-diet-and-cancer-cohort
#5
Björn Fagerberg, Yan Borné, Gerd Sallsten, J Gustav Smith, Stefan Acosta, Margaretha Persson, Olle Melander, Niklas Forsgard, Anders Gottsäter, Bo Hedblad, Lars Barregard, Gunnar Engström
BACKGROUND AND AIMS: Diet and smoking expose the general population to cadmium (Cd), which is a toxic metal that accumulates in the arterial wall. In experimental studies, Cd causes reductions in proliferation of smooth muscle cells and cellular synthesis of procollagen. The aim of this study was to examine whether blood Cd levels, a valid measure of Cd exposure, are associated with increased risk of abdominal aortic aneurysm (AAA). METHODS: All middle-aged men and women enrolled in the Malmö Diet and Cancer study (n = 30 447) were followed from the baseline examination in 1991-1996 through 2009...
April 8, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28445802/nmnat-it-s-an-nad-synthase%C3%A2-it-s-a-chaperone%C3%A2-it-s-a-neuroprotector
#6
REVIEW
Jennifer M Brazill, Chong Li, Yi Zhu, R Grace Zhai
Nicotinamide mononucleotide adenylyl transferases (NMNATs) are a family of highly conserved proteins indispensable for cellular homeostasis. NMNATs are classically known for their enzymatic function of catalyzing NAD(+) synthesis, but also have gained a reputation as essential neuronal maintenance factors. NMNAT deficiency has been associated with various human diseases with pronounced consequences on neural tissues, underscoring the importance of the neuronal maintenance and protective roles of these proteins...
April 23, 2017: Current Opinion in Genetics & Development
https://www.readbyqxmd.com/read/28445792/vitamin-d-supplementation-restores-the-blunted-muscle-protein-synthesis-response-in-deficient-old-rats-through-an-impact-on-ectopic-fat-deposition
#7
Audrey Chanet, Jérôme Salles, Christelle Guillet, Christophe Giraudet, Alexandre Berry, Véronique Patrac, Carla Domingues-Faria, Camille Tagliaferri, Katia Bouton, Justine Bertrand-Michel, Miriam Van Dijk, Marion Jourdan, Yvette Luiking, Sjors Verlaan, Corinne Pouyet, Philippe Denis, Yves Boirie, Stéphane Walrand
We investigated the impact of vitamin D deficiency and repletion on muscle anabolism in old rats. Animals were fed a control (1 IU vitamin D3/g, ctrl, n=20) or a vitamin D-depleted diet (VDD; 0 IU, n=30) for 6 months. A subset was thereafter sacrificed in the control (ctrl6) and depleted groups (VDD6). Remaining control animals were kept for 3 additional months on the same diet (ctrl9), while a part of VDD rats continued on a depleted diet (VDD9) and another part was supplemented with vitamin D (5 IU, VDS9)...
April 8, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28445789/characterisation-of-pb-induced-changes-and-prediction-of-pb-exposure-in-microalgae-using-infrared-spectroscopy
#8
Ly Dao, John Beardall, Philip Heraud
Macromolecular changes in Chlorella sp. FleB1 and Scenedesmus acutus YaA6 exposed to Pb were characterised by Attenuated Total Reflectance-Fourier Transform Infrared (ATR-FTIR) spectroscopy. Spectra were collected in the mid-infrared spectral region and a chemometric approach was used to analyse the spectra. Principal Component Analysis showed that under Pb treatment, carbohydrates and lipids increased while proteins and phosphorylated molecules decreased in both the isolates. These conclusions were corroborated by conventional measurements of photosynthesis and neutral lipids...
April 14, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28445780/mitochondrial-ribosomes-in-cancer
#9
REVIEW
Hyun-Jung Kim, Priyanka Maiti, Antoni Barrientos
Mitochondria play fundamental roles in the regulation of life and death of eukaryotic cells. They mediate aerobic energy conversion through the oxidative phosphorylation (OXPHOS) system, and harbor and control the intrinsic pathway of apoptosis. As a descendant of a bacterial endosymbiont, mitochondria retain a vestige of their original genome (mtDNA), and its corresponding full gene expression machinery. Proteins encoded in the mtDNA, all components of the multimeric OXPHOS enzymes, are synthesized in specialized mitochondrial ribosomes (mitoribosomes)...
April 23, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28445717/hepatic-elovl6-mrna-is-regulated-by-the-gga-mir-22-3p-in-egg-laying-hen
#10
Zheng Ma, Hong Li, Hang Zheng, Keren Jiang, Fengbin Yan, Yadong Tian, Xiangtao Kang, Yanbin Wang, Xiaojun Liu
The elongation of very long chain fatty acids protein 6 (ELOVL6) encodes a fatty acid elongase that is responsible for the final step in endogenous saturated fatty acid synthesis and involves in de novo lipogenesis. Though the regulatory mechanism of ELOVL6 expression has been studied extensively, little is known about the role of miRNA in regulating ELOVL6 gene expression in chicken until now. To investigate the regulatory mechanism of miRNA on the expression of ELOVL6 gene, bioinformatics analysis was employed to predict the potential miRNAs that binding with the 3'untranslated region (3'UTR) of ELOVL6...
April 23, 2017: Gene
https://www.readbyqxmd.com/read/28445700/design-synthesis-of-novel-chitosan-derivatives-bearing-quaternary-phosphonium-salts-and-evaluation-of-antifungal-activity
#11
Wenqiang Tan, Jingjing Zhang, Fang Luan, Lijie Wei, Yuan Chen, Fang Dong, Qing Li, Zhanyong Guo
Two novel chitosan derivatives modified with quaternary phosphonium salts were successfully synthesized, including tricyclohexylphosphonium acetyl chitosan chloride (TCPACSC) and triphenylphosphonium acetyl chitosan chloride (TPPACSC), and characterized by FTIR, (1)H NMR, and (13)C NMR spectra. The degree of substitution was also calculated by elemental analysis results. Their antifungal activities against Colletotrichum lagenarium, Watermelon fusarium, and Fusarium oxysporum were investigated in vitro using the radial growth assay, minimal inhibitory concentration, and minimum bactericidal concentration assay...
April 23, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28445635/synthesis-and-enhanced-corrosion-protection-performance-of-reduced-graphene-oxide-nanosheet-znal-layered-double-hydroxides-composite-film-by-hydrothermal-continuous-flow-method
#12
Xiaohu Luo, Song Yuan, Xinyu Pan, Caixia Zhang, Shuo Du, Yali Liu
Effective prevention of the water, oxygen, and chloride ions held in the hydrotalcite interlayer from diffusing through the layered double hydroxides ( LDH ) layer is crucial importance for its further practical application in the corrosion protection. In this study, a hybrid reduced graphene oxide ( RGO ) nanosheet /Zn2+/Al3+ layered double hydroxides ( RGO/ZnAl-LDH ) composite film with an excellent corrosion protection property on the 6N01 aluminum alloy surface was synthesized by a newly and facile hydrothermal continuous flow method,which can enable direct growth on the substrate...
April 26, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28445477/mitochondrial-respiration-in-highly-aerobic-canines-in-the-non-raced-state-and-after-a-1600-km-sled-dog-race
#13
Benjamin Miller, Karyn Hamilton, Robert Boushel, Katherine Williamson, Verena Laner, Erich Gnaiger, Michael Davis
At the annual Iditarod Race, Alaskan Huskies repeatedly run for up to 8 hours at 16 km/h to complete 1600 km. We previously demonstrated high rates of mitochondrial protein synthesis in Alaskan Huskies, which we suspected allowed rapid remodeling of mitochondrial proteins in response to energetic stress. The purpose of this study was to examine mitochondrial respiration in permeabilized skeletal muscle fibers of Alaskan Huskies in the offseason (Non-raced) and following the 1600 km Iditarod Sled Dog Race (Raced)...
2017: PloS One
https://www.readbyqxmd.com/read/28445411/discovery-of-farnesoid-x-receptor-antagonists-based-on-a-library-of-oleanolic-acid-3-o-esters-through-diverse-substituent-design-and-molecular-docking-methods
#14
Shao-Rong Wang, Tingting Xu, Kai Deng, Chi-Wai Wong, Jinsong Liu, Wei-Shuo Fang
The pentacyclic triterpene oleanolic acid (OA, 1) with known farnesoid X receptor (FXR) modulatory activity was modified at its C-3 position to find new FXR-interacting agents. A diverse substitution library of OA derivatives was constructed in silico through a 2D fingerprint similarity cluster strategy. With further docking analysis, four top-scored OA 3-O-ester derivatives were selected for synthesis. The bioassay results indicated that all four compounds 3 inhibited chenodeoxycholic acid (CDCA)-induced FXR transactivation in a concentration-dependent mode...
April 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28445402/synthesis-of-gibberellic-acid-derivatives-and-their-effects-on-plant-growth
#15
Hao Tian, Yiren Xu, Shaojin Liu, Dingsha Jin, Jianjun Zhang, Liusheng Duan, Weiming Tan
A series of novel C-3-OH substituted gibberellin derivatives bearing an amide group were designed and synthesized from the natural product gibberellic acid (GA₃). Their activities on the plant growth regulation of rice and Arabidopsis were evaluated in vivo. Among these compounds, 10d and 10f exhibited appreciable inhibitory activities on rice (48.6% at 100 μmol/L) and Arabidopsis (41.4% at 100 μmol/L), respectively. These results provide new insights into the design and synthesis of potential plant growth regulators...
April 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28445324/nurse-practitioner-physician-comanagement-of-primary-care-patients-the-promise-of-a-new-delivery-care-model-to-improve-quality-of-care
#16
Allison Andreno Norful, Kyleen Swords, Mickaela Marichal, Hwayoung Cho, Lusine Poghosyan
BACKGROUND: The U.S. primary care system is under tremendous strain to deliver care to an increased volume of patients with a concurrent primary care physician shortage. Nurse practitioner (NP)-physician comanagement of primary care patients has been proposed by some policy makers to help alleviate this strain. To date, no collective evidence demonstrates the effects of NP-physician comanagement in primary care. PURPOSE: This is the first review to synthesize all available studies that compare the effects of NP-physician comanagement to an individual physician managing primary care...
April 25, 2017: Health Care Management Review
https://www.readbyqxmd.com/read/28445169/continuous-size-and-shape-control-synthesis-of-hollow-silica-nanoparticles-enabled-by-a-microreactor-assisted-rapid-mixing-process
#17
Yujuan He, Ki-Joong Kim, Chih-Hung Alex Chang
Hollow silica nanoparticles (HSNPs) were synthesized using a microreactor-assisted system with a hydrodynamic focusing micromixer (HFM). Due to the fast mixing of each precursor in the system, the PAA thermodynamic-locked (TML) conformations were protected from their random aggregations by the immediately initiated growth of silica shells. When altering the mixing time through varying flow rates and flow rate ratios, the different degrees of the aggregation of PAA TML conformations were observed. The globular and necklace-like TML conformations were successfully captured by modifying the PAA concentration at the optimized mixing condition...
April 26, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28445152/multiplexed-gene-expression-profiling-identifies-the-fgfr4-pathway-as-a-novel-biomarker-in-intrahepatic-cholangiocarcinoma
#18
Changhoon Yoo, Jihoon Kang, Deokhoon Kim, Kyu-Pyo Kim, Baek-Yeol Ryoo, Seung-Mo Hong, Jung Jin Hwang, Seong-Yun Jeong, Shin Hwang, Ki-Hun Kim, Young-Joo Lee, Klaus P Hoeflich, Oleg Schmidt-Kittler, Stephen Miller, Eun Kyung Choi
BACKGROUND: The fibroblast growth factor receptor 4 (FGFR4) pathway is an essential regulatory component of bile acid synthesis, and its relationship with hepatocellular carcinoma (HCC) has been reported. We investigated the gene expression and clinical significance of FGFR4 and related pathways in intrahepatic cholangiocarcinoma (iCCA). RESULTS: The median age was 56 years (range 30-78) and 34 patients (74%) were male. Six patients (13%) had hepatitis B virus infection, with or without liver cirrhosis...
April 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28445072/an-approach-to-the-core-of-lactonamycin
#19
Philip J Parsons, Daniel R Jones, Lee J Walsh, Lewis A T Allen, Ada Onwubiko, Lewis Preece, Johnathan Board, Andrew J P White
A cascade reaction has been developed for the synthesis of lactonamycin. In this paper, we demonstrate that a transition-metal-free thermal ene-diyne cyclization can be used for the construction of the entire core of the antibiotic lactonamycin and anticancer agent lactonamycin Z.
April 26, 2017: Organic Letters
https://www.readbyqxmd.com/read/28445071/polymorphic-assembly-from-beveled-gold-triangular-nanoprisms
#20
Juyeong Kim, Xiaohui Song, Fei Ji, Binbin Luo, Nicole F Ice, Qipeng Liu, Qiao Zhang, Qian Chen
The shape anisotropy of nanoparticle building blocks is of critical importance in determining their packing symmetry and assembly directionality. While there has been extensive research on the effect of their overall geometric shapes, the importance of nanometer morphology details is not well-recognized or understood. Here we draw on shape-anisotropic gold triangular nanoprism building blocks synthesized based on a method we recently developed; besides the "large-scale" triangular prism shape (79.8 nm in side length and 22...
April 26, 2017: Nano Letters
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