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Studies on FXR knockout mice demonstrated that FXR
2022-06-14

Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.
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Recently a lot of synthetic FFA agonists containing acidic
2022-06-14

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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rotenone Species specificity of small molecular
2022-06-14

Species specificity of small molecular GPR40 agonists have been reported by Takeda scientist. In the binding pocket of TM5, a Leu186 in human GPR40/FFA1 is replaced with Phe in rat, resulting in dramatic inter-species GPR40 activity discrepancy in certain scaffolds of small molecular GPR40 agonists.
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The anti platelet functions of ZGR were confirmed by
2022-06-14

The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati
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br Anandamide signaling and cardiovascular function The card
2022-06-14

Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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SAG It should be noted that
2022-06-14

It should be noted that the current studies were performed in female rats. Although the oestrous cycle has been shown to modulate inflammatory processes in the periphery, data from our group has demonstrated that the phase of the oestrus cycle does not significantly alter TLR3-mediated neuroinflamma
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br Main Text Metabolism drives diverse
2022-06-13

Main Text Metabolism drives diverse biological processes including differentiation, proliferation, and effector function in diverse cell types. In particular, the process of mounting an innate immune response to pathogens entails rapid sensing of a wide range of patterns displayed by invading mic
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In order to study the role
2022-06-13

In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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br Pathophysiology of glaucoma Glaucoma is a group
2022-06-13

Pathophysiology of glaucoma Glaucoma is a group of optic neuropathies defined by progressive degeneration of RGCs and their SC 144 synthesis in the optic nerve, which leads to irreversible loss of vision [3,8,9]. RGC degeneration is often significantly advanced before changes in visual acuity an
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br Acknowledgements br Introduction The glutathione S
2022-06-13

Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and co
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br Conclusion In conclusion we showed
2022-06-13

Conclusion In conclusion, we showed that apoptosis is involved in etoposide-induced pancreatic β-cell cytotoxicity. More importantly, as shown in Fig. 6, the results of this study demonstrated that etoposide induces pancreatic β-cell death via the JNK/ERK activation-mediated GSK-3 downstream-trig
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GPR has been implicated in
2022-06-13

GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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The ER is responsible for calcium storage
2022-06-13

The ER is responsible for calcium storage, lipid and protein biosynthesis, and the folding, assembly, and maturation of proteins [23], and ER stress is one of the main causes in T2DM, which leads to β-cell apoptosis and dysfunction [[5], [6], [7]]. In this study, TG was used as an ER stress inducer.
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Further our study provides the first evidence that zaprinast
2022-06-13

Further, our study provides the first evidence that zaprinast and kynurenic serine protease administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effective anal
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DTP3 australia In order to investigate whether this off targ
2022-06-13

In order to investigate whether this off-target activity was related to a particular structural feature of this DTP3 australia or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups,
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