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During the course of the
2022-01-17

During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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br Materials and methods br Results
2022-01-17

Materials and methods Results Discussion Zn2+ is an extremely abundant transition metal in the synaptic vesicles of hippocampal glutamatergic mossy fibers and remains a key factor in the modulation of neuronal plasticity (Assaf and Chung, 1984). Disruption of Zn2+ homeostasis is associated
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GSK2126458 Studies on FXR knockout mice
2022-01-17

Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.
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Data are expressed as means SE Statistical significance was
2022-01-15

Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of U87MG PD173955 expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, insert).
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In cardiomyocytes mechanical stress builds up via FAs and
2022-01-15

In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a tran
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br Hippo Signaling in Autoimmunity An imbalance of T cell
2022-01-15

Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T NMS-873 (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg differentiation
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br Acknowledgments This research was partially supported by
2022-01-15

Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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br Discovery of GPR A The murine niacin receptor protein
2022-01-15

Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t
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Our overall goal is to
2022-01-15

Our overall goal is to develop selective compounds for low-affinity/high-capacity transporters inhibitors (i.e. OCT1–3 and PMAT), and provide the field with much needed, specific pharmacological tools to study these transporters. In our initial efforts, we synthesized halogen substituted analogs and
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PBI is an agonist of GPR and acts as
2022-01-15

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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Therefore we investigated the acute and delayed response of
2022-01-15

Therefore, we investigated the acute and delayed response of 92 human mono- and dizygous twins to an acute shift from low fat to high fat diet with respect to serum levels of VEGF and the expression of SLC2A1 in subcutaneous adipose tissue (AT). By comparing the degree of concordance of basal and di
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GK also called hexokinase IV or D is a
2022-01-15

GK, also called hexokinase IV or D, is a glycolytic enzyme that converts dapagliflozin receptor to glucose-6-phosphate. GK has unique characteristics compared with those of the ubiquitously expressed hexokinase isoforms I–III, and is predominantly expressed in the pancreas and liver. In pancreatic
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br Experimental br Results br
2022-01-15

Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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However ghrelin has a short half life
2022-01-15

However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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br Funding This work was supported by the National
2022-01-15

Funding This work was supported by the National Institutes of Health (RO1DK097550 to JT, RO1AG046619 to WAB and TS, and T32AG000057 to EMR, and T32DK007012 to SG) and by the Veterans Affairs Puget Sound Health Care System Research and Development. Introduction In mammals, two isoforms of grow
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