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Introduction The onset of uterine labor is
2021-10-22

Introduction The onset of uterine labor is the culmination of a gradual uterine activation wherein physiological inflammation induces a common prolabor pathway characterized by increased myometrial contractility, weakening of fetal membrane integrity, and cervical ripening. Pathological proinflamma
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In the present study we showed
2021-10-22

In the present study, we showed that reduced neuron formation in vitro induced by IL-1β was ameliorated by activation of GPR55 in both human and mouse cultures of NSCs. Pre-treatment with GPR55 agonists also blocked upregulation of inflammatory cytokine receptor mRNA (IL-1R1, IL-6st) while increasin
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Among the compounds prepared at
2021-10-22

Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with moderat
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To investigate if such an effect
2021-10-22

To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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Next we investigated the accumulation of H
2021-10-22

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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In the present study five Glu substituted analogues of GIP
2021-10-22

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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These reports have gradually established G quadruplex bindin
2021-10-21

These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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Fatty acids are also known to
2021-10-21

Fatty acids are also known to activate G-protein coupled receptors (GPCRs). LCFAs activate the GPCRs for free fatty 5-(N,N-dimethyl)-Amiloride hydrochloride (FFA)1 and FFA4 (Briscoe et al., 2003; Hirasawa et al., 2005), whereas SCFAs activate FFA2 and FFA3 receptors, which are expressed in bovine n
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Danazol Natural product based drug discovery
2021-10-21

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Danazol binding assays, we used molecular modeling to predict how well these compounds fit
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Contrary to the transient nature
2021-10-21

Contrary to the transient nature of signal transmission through PLCβ, genome-wide RNAi screens revealed that the signaling events driven by Gαq that result in aberrant cell proliferation depends on highly specific protein-protein interactions, rather than solely on diffusible second messenger system
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br New design of an HIF injector Since the
2021-10-21

New design of an HIF injector Since the invention of RFQ, RFQ-based 1 GW HIF plans have been proposed in Japan, Europe and the Soviet Union, such as HIBALL, HIDIF and HIBLIC. In these plans, driver linacs were numerous, huge and complicated. Considering the space-charge-effect of the intense heav
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OS has a key role in the
2021-10-21

OS has a key role in the pathogenesis of micro- and macrovascular diabetic complications [3]. There is now convincing evidence that the enzymes that generate ROS and gasotransmitters, such as nitric oxide (NO) and CO, are redox regulated at both the transcription and activity levels, and are also im
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br Conclusion Until recently astrocytes were recognized sole
2021-10-21

Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of Celecoxib homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In particular, gli
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br Introduction Cherry tomato Solanum lycopersicum L
2021-10-21

Introduction Cherry tomato (Solanum lycopersicum L.) is a commonly consumed fruit on a worldwide scale due to its characteristic flavor and high nutrition (Wei et al., 2016, Yu et al., 2014). Tomato is low in fat and calories, and is a rich natural source of nutrition and bioactive antioxidant co
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br Introduction Calorie restriction CR in the absence of mal
2021-10-21

Introduction Calorie restriction (CR), in the absence of malnutrition, has beneficial effects on src inhibitor function, including reducing the incidence of age-related neurodegenerative disease (Gräff et al., 2013), eliciting anti-depressant behavior (Lutter et al., 2008) and improving memory f
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