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With the identification of small
2021-12-17
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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Although our knowledge of how FAs affect GLP producing L
2021-12-17
Although our knowledge of how FAs affect GLP-1-producing L-cells is sparse and incomplete, increased intracellular ceramide [6], ER stress [12], and increased production of ROS [9] are indicated mediators of the lipotoxicity induced by SFA (16:0). However, the role for/interaction between these medi
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lgk974 In this study we intended to explore the efficacy
2021-12-17
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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More specific quantitative assays for DiXaIs are
2021-12-17
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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Lastly the N position of this privileged
2021-12-17
Lastly, the N-1 position of this privileged pyrimidone was further substituted by a variety of different aromatic, aliphatic or heteroaromatic linkers with carbonyl functionality. In this task, different N-1 substituted pyrimidones 20i–20xiv were generated and check against HIV IN 3′-processing and
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PIK-III One limitation of our study
2021-12-17
One limitation of our study was that all control dogs had histologic evidence of mild GI inflammation according to established WSAVA guidelines (Washabau et al., 2010), despite being apparently healthy purpose-bred research dogs housed in a controlled environment with no history of vomiting, diarrhe
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The identity of organelles is defined by a particular set
2021-12-17
The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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A second feature of the Ras type GTPases is that
2021-12-17
A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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br Conclusion br Conflict of interest
2021-12-17
Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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Bufalin Fourthly the distribution sites after i c v injectio
2021-12-17
Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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SB 216763 In the present study we also found that specificit
2021-12-17
In the present study, we also found that specificity concerns persist for antibody-based tools, like ELISAs. Measuring the same human plasma sample with four different commercial galanin ELISA kits produced four widely different galanin concentrations. No recovery of synthetic galanin peptide added
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br Conclusion Discovery of an ideal orally
2021-12-16
Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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The ETA receptor has a higher
2021-12-16
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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Smoking is strongly and consistently associated with periodo
2021-12-16
Smoking is strongly and consistently associated with periodontitis in the general population. In our study we detected a similar pattern in patients with HIV infection: smokers had a higher DPSI score compared to non-smokers. The exact cause of smoking as a risk factor for periodontitis in the gener
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Sometime ago we have described
2021-12-16
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by BV6 and zymosan. In this work we describe new derivatives
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