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To develop novel EPAC inhibitors Zhou and co workers
2020-07-11

To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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Although MMP might be a downstream target
2020-07-11

Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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Despite the important agronomic traits regulated by SUMO
2020-07-10

Despite the important agronomic traits regulated by SUMO, most research studies on SUMOylation have been mainly limited to model plants, such as Arabidopsis and rice (Wang et al., 2011), due to the lack of molecular tools specific to other economically relevant plants. On the other hand, plants harb
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br Materials and methods br Results
2020-07-10

Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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polymyxin sulfate Sp family protein has been
2020-07-10

Sp family protein has been regarded as the housekeeping gene and is ubiquitously expressed. Although Sp family expression is regulated with some stimuli [17], [20], the total Sp family protein levels are not changed in most cases, as observed in our present study (Fig. 4). Constitutive binding of th
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The overall poor outcomes in ESCC are thought because of
2020-07-10

The overall poor outcomes in ESCC are thought because of a combination of late diagnosis, aggressiveness of the disease, and a lack of effective treatment strategies for systemic disease. Several molecular pathways, such as epidermal growth factor receptor, vascular endothelial growth factor, and p5
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Introduction Cytochrome P CYP A is
2020-07-10

Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The PF-04620110 level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A
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Flexible alignment of isopropylphenylaminobenzimidazole with
2020-07-10

Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead ionophore 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other key funct
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Introduction Robust evidence suggests that genetic
2020-07-10

Introduction Robust evidence suggests that genetic factors influence an individual\'s susceptibility to BD (Craddock and Sklar, 2013). Yet, no single, high penetrance gene has been identified with direct causality (Craddock and Sklar, 2009). The largest GWAS to date for identifying genes conferring
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In different body organs a number of biological
2020-07-10

In different body organs, a number of biological functions are generally mediated by binding of the extracellular substances to the particular transmembrane receptors, which results in subsequent signal stimulation by intracellular signaling cascades. These cascades function over the complex network
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There are conflicting studies on ET axis and its relationshi
2020-07-10

There are conflicting studies on ET axis and its relationship with clinicopathologic parameters in various cancers. Endothelin axis expression in the tissue and in blood has been associated with advanced cancer characteristics in colorectal, breast, and prostate cancer, while showing no linkage to c
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Mexiletine HCl receptor A widely accepted mechanism to diffe
2020-07-09

A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the Mexiletine HCl receptor [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is piv
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3mb We then analyzed Ki proliferation index
2020-07-09

We then analyzed Ki-67 proliferation index as a categorical variable by using 15%, essentially the median Ki-67 value in the entire study group (see above), to delineate low and high proliferation subgroups. By Fisher\'s exact test, both the type 1 versus non-type 1 EWS-FLI1 comparison (P = 0.047; T
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br Materials and methods br
2020-07-09

Materials and methods Results Discussion Cisplatin, as one member of a class of platinum-containing anti-cancer drugs, which displays a great deal of clinical activity on a wide variety of solid tumors. In addition, cisplatin often used in combination with other chemotherapy drugs to treat
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In the horse oviduct the EP receptor
2020-07-09

In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial pdk 1 particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects differences in
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