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Among the compounds prepared at this stage
2021-09-27

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 modera
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Overall ABC transporters are hypothesised to prevent the pen
2021-09-27

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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Cy3 hydrazide With these cyclopropene glutamate derivatives
2021-09-27

With these cyclopropene-glutamate derivatives in hand, we tested their ability to ligate with popular bioorthogonal reagents (Fig 3). First, we tested their ability to ligate with a tetrazine (3,6-Di-2-pyridyl-1,2,4,5-tetrazine) via an inverse electron demand Diels-Alder reaction by monitoring the c
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We report here a patient with
2021-09-26

We report here a patient with a one-base frame-shift deletion in the PURA gene that presented an unusual phenotype including persistent hypoglycorrhachia. We propose a possible link between hypoglycorrhachia and PURA dysfunction postulating PURA as a GLUT1 regulator. We therefore hypothesize that mu
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Cx mimetic peptides short synthetic peptides
2021-09-26

Cx mimetic peptides, short synthetic peptides corresponding to intracellular amino Kaempferol-3-rutinoside sequences of diverse Cx have better specificity compared to traditional GJ blockers and openers. In particular, it was reported that Cx mimetic peptides reversibly inhibited GJ channel function
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Similar to C lividipennis RDL Jiang et
2021-09-26

Similar to C. lividipennis RDL (Jiang et al., 2015), we found that the intracellular loop variants of A. mellifera RDL had no effect on GABA EC50 (Table 1). Also, as with C. lividipennis, there was no significant difference in maximal GABA responses (Table 1). However, whereas the 31 amino acid inse
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However Gingrich and Hen reported that absence of the gene
2021-09-26

However, Gingrich and Hen reported that absence of the gene at all stages of ontogenesis of mice may interfere with the normal developmental program and/or the organism may undergo changes in other systems to compensate for gene absence (46). In addition, potentially altered maternal behavior of GPR
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These observations are of particular
2021-09-26

These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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Although angiogenesis is crucial for cerebral ischemic rehab
2021-09-26

Although angiogenesis is crucial for cerebral ischemic rehabilitation, the mechanism underlying NGF promotion of angiogenesis is not clear. Previous studies showed that angiogenesis can be promoted by FAK, in a breast cancer model [19]. Recent studies showed that FAK phosphorylation participated in
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br Experimental br Results and discussion One
2021-09-26

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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By association a possible mechanism
2021-09-26

By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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In total strains with relatively rapid acid
2021-09-26

In total, 5 strains with relatively rapid acid-producing ability (MA14, 15M2, DQHXNQ38–12, 5G2, and 6G5) were selected for further analysis. Compared with the strains ATCC19435, ZN8, and D-XJ4–12, which were used as controls, these 5 strains exhibited significantly different growth and titratable ac
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Compared to a large database of
2021-09-26

Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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The Hippo pathway is a
2021-09-26

The Hippo pathway is a growth control signaling cascade that has been demonstrated to play an important role in regulating cell proliferation and differentiation [5,6]. The core signaling pathway consists of a group of kinases which negatively regulate the expression of transcriptional co-activators
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Lastly certain populations of immune cells may
2021-09-26

Lastly, certain populations of immune cells may be Hh responsive. Although PC have not been demonstrated in healthy liver-resident macrophages or lymphocytes, macrophages in injured livers have been shown to produce Hh ligands[58], [100], [101] and treating liver-derived macrophages with neutralisin
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