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br Introduction L Glutamate is one of the
2022-02-18
Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of BET bromodomain inhibitor functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At ele
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Herein we report the discovery of AM
2022-02-18
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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br Methods br Results br Discussion In this
2022-02-18
Methods Results Discussion In this series of studies we hypothesized that FHH-GHSRm1/Mcwi rats would, relative to their WT counterparts, exhibit a metabolic and behavioral phenotype reminiscent of GHSR−/− mice. Through the use of the GHSR−/− mouse, a great deal about the role of ghrelin sig
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p2y receptor br General features of FGFRs and inhibitors
2022-02-18
General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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br Conclusions GPCRs are versatile signaling molecules regul
2022-02-18
Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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PBI is an agonist of
2022-02-18
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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To enhance the impact of
2022-02-18
To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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Cy5.5 NHS ester Introduction The Antiretroviral Therapy ART
2022-02-18
Introduction The Antiretroviral Therapy (ART), in the last decade, has been providing a better treatment for the Human Immunodeficiency Virus 1 (HIV) infection, by reducing its viral load to undetectable levels and recovering the immune system. In fact, according to the last data from UNAIDS the mo
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Biliary tract cancers BTC are categorized into
2022-02-18
Biliary tract cancers (BTC) are categorized into intrahepatic, perihilar, extrahepatic BTC (or cholangiocarcinoma) as well as gallbladder cancer (GBC). Although the incidence of BTC is low in developed countries (3% of gastrointestinal cancers), BTC is the second most common primary liver tumor afte
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In our study SHH protein overexpression was significantly
2022-02-17
In our study, SHH protein overexpression was significantly associated with lymph node metastasis which is in agreement with the study done by Marechal et al. wherein they have reported that SHH is a prognostic biomarker in PDAC and high levels correlate with lymph node metastasis (Maréchal et al., 2
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In order to determine whether NF B
2022-02-17
In order to determine whether NF-κB could interact with GSTP1-1 promoter, we performed EMSA. One NF-κB like (−98κB) binding site was previously described in the GSTP1-1 promoter as a regulator element. However, few data about this site have been published and its role in the GSTP1-1 gene regulation
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The timing and growth of follicles
2022-02-17
The timing and growth of follicles relative to follicle deviation was assessed in 49 cows (Fig. 4) that had NFWE following treatment onset and that had not already established dominance. Because day of deviation did not differ due to treatment, day of estrous cycle, or replicate, data are presented
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br STAR Methods br Introduction Glycosylation
2022-02-17
STAR★Methods Introduction Glycosylation is one of the most prevalent post-translational modifications of proteins. It not only plays major roles in folding, transport and localization of proteins [1], but also regulates various biological processes such as cell growth, viral replication and im
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Ironically another series of studies examining the role
2022-02-17
Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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Although both receptors mGluR and mGluR are
2022-02-17
Although both receptors, mGluR1 and mGluR5, are present in cortical and hippocampal areas from 1 to 2 weeks old neonates (López-Bendito et al., 2002) we have found that only mGluR1 was regulated after maternal l-Glu consumption. A possible explanation could be based on the different ontogenetic prof
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