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High lipophilicity of seems to cause poor
2021-10-13
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine in th
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br Methods and materials br Results br Discussion In this
2021-10-13
Methods and materials Results Discussion In this study we demonstrate that CF epithelial aphidicolin exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsible for t
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The organ culture method has previously shown
2021-10-13
The organ culture method has previously shown to be a suitable model for investigations of receptor upregulation on vascular smooth muscle cells (Adner et al., 1996). In our study, the organ culture method was applied in order to examine whether LPS from P.g. was capable of altering the gene express
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BMP signals play pivotal roles in the various processes of
2021-10-13
BMP signals play pivotal roles in the various processes of chondrogenesis [12], [13]. At early stages of chondrogenesis, BMP signaling regulates the differentiation of mesenchymal NPS-2143 into chondrocytes via the induction of Sox9[29]. The loss of Noggin, a BMP antagonist, results in the overgrow
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SCH is a H R receptor
2021-10-13
SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese
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br Dynamic Localization of Hippo Pathway Components
2021-10-13
Dynamic Localization of Hippo Pathway Components The observation that Wts normally localizes with an inhibitor, Jub, raised the question of how and where Wts normally becomes activated. Under conditions of pathway activation in Drosophila imaginal discs, Wts relocalized from Jub to Ex, where it i
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Cdc is also linked to the adherens junction via
2021-10-13
Cdc42 is also linked to the adherens junction via IQGAP1, however, it appears to have an opposite effect on junctional stability. When Cdc42 is inactive, IQGAP1 binds to β-catenin, displacing α-catenin, resulting in the loss of α-catenin-linked DCG IV filaments from the adherens junction and reduce
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acetylcholine receptors One of the most common dietary
2021-10-13
One of the most common dietary approaches against obesity-associated diseases is the increase in the consumption of ω3 polyunsaturated fatty acids [18], [19]. Since seminal paper by Bang and Dyeberg in which the low prevalence of coronary heart disease among the Inuit was associated with the high ma
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GPR is a member of
2021-10-13
GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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In this study we describe the role
2021-10-13
In this study, we describe the role of a specific species of LPI in the secretion of GLP-1 from enteroendocrine L-cells and primary cell preparations. We further demonstrate the specific role of GPR119 in LPI-dependent GLP-1 secretion. To achieve this, we downregulated GPR119 and GPR55 protein expre
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Introduction Nicotinic acid niacin NA has been used in the
2021-10-13
Introduction Nicotinic po1 synthesis (niacin, NA) has been used in the treatment of dislipidemia and cardiovascular disease for almost 60years (Offermanns, 2006). Large clinical studies showed that niacin alone or in combination with LDL-lowering drugs improved cardiovascular outcomes (Canner et al
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Poziotinib Following activation it is necessary for
2021-10-13
Following activation, it is necessary for a subset of activated effector T cells to survive as long-lived memory T cells. Metabolically, this transition is dependent upon the ability of the cell to downregulate aerobic glycolysis and transition back to a more oxidative phenotype. In fact, enhancemen
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br Methods and materials br Acknowledgements The
2021-10-13
Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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Glycogen synthase kinase GSK is currently considered to
2021-10-13
Glycogen synthase kinase 3 (GSK3) is currently considered to be a multifunctional serine/threonine kinase involved in a wide spectrum of cellular processes such as glycogen metabolism, cell proliferation, neuronal function, oncogenesis or embryonic development (for recent reviews see: Rayasam et al.
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Four polymorphic variants of Neil namely S
2021-10-13
Four polymorphic variants of Neil1, namely, S82C (rs5745905), G83D (rs5745906), C136R (rs5745907) and D252N (rs5745926) were characterized by Roy et al. in 2007 (Table 1). Analyses of AP site incision on Tg containing oligonucleotide showed that S82C and D252N variants had wild type activity and car
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