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However at variance with the well studied R form of
2022-08-03
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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Atglistatin The molecular target of N
2022-08-03
The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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This SAR work led to the identification
2022-08-03
This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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MI-773 Recent efforts have also tried to identify cancer sub
2022-08-03
Recent efforts have also tried to identify cancer subsets that are exquisitely responsive to EZH2i apart from those bearing EZH2 gene mutation (Knutson et al., 2012). The dysfunction of SWI-SNF complex, a chromatin-remodeling regulator that partially antagonizes the catalytic function of PRC2 comple
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The strict control of Spi expression is
2022-08-03
The strict control of Spi1 expression is critical for proper myeloid cell fate determination, and genetic or epigenetic changes in the Spi1 gene frequently contribute to the leukemogenesis in mice and human. It is has been shown that Spi1 expression is frequently downregulated in human AML patients
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2881 Materials and methods br Results and
2022-08-03
Materials and methods Results and discussions Conclusions In this study, we identified 7 histone acetyltransferases and 12 histone deacetylases in Marchantia polymorpha. The present phylogenetic analysis of MpHATs and MpHDACs provide the insight into the evolutionary relationships of these tw
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Fig summarizes the results for M
2022-08-03
Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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br Tissue Specific Roles for HIF PHD Isoforms Hypoxia
2022-08-03
Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune vx 20 sale and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory co
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The increased levels of proinflammatory cytokines in BALF
2022-08-03
The increased levels of proinflammatory cytokines in BALF are noted during ALI/ARDS, and the persistent elevation of these mediators may exaggerate systemic or focal inflammatory reaction with a worse outcome. These cytokines, particularly TNF-α and IL-6, play essential roles in ALI [16,17]. The ove
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NAD+ br TGR agonists current developments and future landsca
2022-08-02
TGR5 agonists: current developments and future landscape The amphipathic nature of bile acids is crucial in aiding the digestion and NAD+ of vitamins and fats. With the emerging roles of bile acids in the regulation of energy and glucose homeostasis through TGR5, the pharmaceutical industry has
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In parallel we were also
2022-08-02
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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Depending upon the varied habitats e g soil water
2022-08-02
Depending upon the varied habitats (e.g. soil, water, animal digestive tracts, etc.), microbes possess a diverse range of carbohydrate ABC transporters and metabolic pathways (Rodionov et al., 2013; Bräsen et al., 2014). Thermus thermophilus HB8, a thermophilic gram-negative bacterium dwelling in ho
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Introduction Adaptations in the metabolism
2022-08-02
Introduction Adaptations in the metabolism of cancers contribute to tumor survival and growth and present opportunities to develop novel therapeutic strategies (Kelloff et al., 2005, Som et al., 1980). In particular, glutamine metabolism plays such an important role in cancer growth that a phenomen
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In order to discover novel small
2022-08-02
In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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br STAR Methods br Acknowledgments
2022-08-02
STAR★Methods Acknowledgments We would like to thank Dr. Xiping Cheng for help with the immunohistochemistry staining, Qi Su for help with gene expression analysis, and Dr. Chaoying Liang at the UTSW Genomics Microarray Core facility for assistance on RNA-seq. W.-H.L. was supported by grant awa
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