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20b As natural ligands of GPR several long chain
2022-02-01
As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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In addition to these effects on metabolic
2022-02-01
In addition to these effects on metabolic function in cardiac cells, this study also demonstrates changes in the expression of hypertrophic genes and proteins subsequent to GPR119 activation. Again this occurred in a distinct pattern dependent on palmitate exposure. Of interest SOCS3 mRNAs were decr
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Disrupting the dialog between microbiota and the host especi
2022-02-01
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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Armed with this knowledge we
2022-02-01
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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In respect of clinical development Takeda has pioneered the
2022-02-01
In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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Prior to cellular uptake studies of compound docking simulat
2022-02-01
Prior to cellular uptake studies of brincidofovir , docking simulation was performed (A). The result suggested this complex was capable of binding in the cavity of an outward open XylE. The orientation of the sugar moiety in the docked complex was similar to that of the glucose unit bound in the cr
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74 9 To maintain low Glu concentrations in the synaptic clef
2022-02-01
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino 74 9 is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in to a
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With the identification of small
2022-01-31
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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Type II diabetes is characterized
2022-01-31
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty ALW-II-41-27 sale receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors and
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In summary PPARG and FFAR are
2022-01-31
In summary, PPARG and FFAR1 are connected in several ways, and the presented interaction is mechanistically reasonable. Additional investigations are required to elucidate the exact details of the underlying physiology. However, our findings are of immanent importance for the treatment of type 2 dia
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Based on the inhibitory potency of C
2022-01-31
Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o
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The top panel of Fig depicts the average number of
2022-01-31
The top panel of Fig. 3 depicts the average number of planaria visible during each observation for all cohorts in the group testing following light exposure. Although there was considerably more variability than in the light-exposure conditions, a t-test showed no significant difference in count be
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In this study we also profiled the expression of the
2022-01-31
In this study, we also profiled the expression of the transporters in wild-type RBL-2H3 cells, RBL-2H3 Sc98 cells, and rat peritoneal mast cells. OCT1 and PMAT were expressed at high levels in both RBL-2H3 Sc98 and RBL-2H3 cells. However, OCT2 and OCT3 were weakly or least detected in RBL-2H3 Sc98 c
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The standard model of stress postulates
2022-01-30
The standard model of stress postulates the activation of both the sympathoadrenomedullary axis and the hypothalamo-pituitary-adrenocortical axis. Long-term activation of either neuroendocrine axes has been shown to be harmful [12]. Short-term activation of the sympathoadrenomedullary axis is used t
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br Materials and methods br Results br Discussion Since
2022-01-29
Materials and methods Results Discussion Since early times, herbs and their extracted substances have been used as foods and medicinal resources worldwide (Petrovska, 2012). A Ginger is one of the most important and oldest spices, consisting of the prepared and sun-dried rhizomes of Zingibe
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