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In summary we have identified a series of amides
2019-10-10

In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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For the current studies we used the selective Epac
2019-10-10

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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Previously we have described increased expression
2019-10-10

Previously, we have described increased expression of both cytokine and chemokine mRNA (e.g. MCP-5 and fractalkine) in the left ventricle of male EP4-KO mice with dilated cardiomyopathy [2]. Takayama et al. [31] have shown that PGE2 potently inhibits cytokine/chemokine secretion (MCP-1, interleukin
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AMPHs facilitate dopamine release which further triggers dop
2019-10-09

AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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Inopportunely normal aging brings about decreases in
2019-10-09

Inopportunely, normal aging brings about decreases in frontal D1 receptor densities and a gradual decline in postsynaptic markers of dopamine in striatal, neocortical, and limbic areas of the D-Mannitol mass (Bäckman et al., 2006, de Keyser et al., 1990, Karrer et al., 2017, Suhara et al., 1991, Wa
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br Other pathways involved in the preventive and
2019-10-09

Other pathways involved in the preventive and therapeutic potential of flavonoids in neurodegenerative diseases Rather than the induction of MAPK/ERK pathway, flavonoids actively modulate other critical intracellular neuronal survival and death protein kinases pathways, more importantly PI3K/Akt,
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WNV a member of the
2019-10-09

WNV, a member of the genus Flavivirus within the family Flaviviridae, was first isolated in 1937 from a febrile woman in the West Nile region of Uganda (Brinton, 2002). Until 1999, WNV was mainly confined to Southern Europe, the Middle East, Africa, West and Central Asia, Indonesia and Australia. In
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Acknowledgments br Introduction Diabetes mellitus DM is
2019-10-09

Acknowledgments Introduction Diabetes mellitus (DM) is a multifactorial disease [1] associated with serious comorbidities. This condition has recently reached epidemic proportions, as its occurrence has exponentially increased in the general population. Over 400 million people worldwide were est
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In attempts to further purify His
2019-10-09

In attempts to further purify [His]6-Artemis, numerous matrices were assessed including anion and cation exchange, and SU5416 interaction chromatography. The results from these matrices were universally poor (data not shown). Fractionation via adsorption chromatography on a hydroxyapatite (HAP) mat
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In studies directed toward the
2019-10-09

In studies directed toward the development of sequence-specific major-groove binding small NAD+ [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and affinit
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Enzyme mimics belong to a type
2019-10-08

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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We can think of two ways in which collagen binding
2019-10-08

We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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Oysters belong to the second largest animal phylum Mollusca
2019-10-08

Oysters belong to the second largest animal phylum Mollusca, and they are globally distributed aquaculture animals (Wang et al., 2018). A number of studies have demonstrated that oysters have evolved an integrated and complex innate immune system to recognize and eliminate various invaders. An array
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Several functions of FAT have been suggested
2019-10-08

Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer igf ir overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006). In other studies,
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The CysLT receptor antagonist BayCysLT RA significantly supp
2019-10-08

The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear meclofenamate into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Barret et
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