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In the course of our synthetic studies we also discovered
2022-04-12
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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br Materials and methods br Conflicts of interest Some of
2022-04-12
Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He
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Many investigators have noted structural
2022-04-12
Many investigators have noted structural similarities between certain flavonoids and benzodiazepines, such as diazepam, that are the most widely studied positive modulators of GABAA receptors. Benzodiazepines can act on these receptors via ‘two distinct and separable mechanisms’ (Walters, Hadley, Mo
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In addition to indoles two additional structural variants we
2022-04-11
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic N1-Methyl-ATP side chain to prepare compound (). The extension of the chain
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br The HDC knockout mouse
2022-04-11
The HDC knockout mouse as a pathophysiological model of TS The implication of a hypomorphic allele of the Hdc gene as a rare cause of TS (Ercan-Sencicek et al., 2010) created a rare opportunity for the generation of a pathophysiologically grounded model of the disorder. Modeling pathophysiology o
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br Discussion Our results showed that the
2022-04-11
Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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Numerous strategies of cardiomyocyte protection are effectiv
2022-04-11
Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].
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br Activity dependent control of myelination and myelin main
2022-04-11
Activity-dependent control of myelination and myelin maintenance Oligodendrocytes have intrinsic myelinating capacity and can myelinate fixed glatiramer acetate in addition to synthetic nanofibers and micropillars [21, 34, 35]. What prevents oligodendrocytes from myelinating dendrites or other c
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To determine the functional consequences of HIV gp
2022-04-11
To determine the functional consequences of HIV gp120 binding to vaginal epithelial cells, an annotation clustering of the differentially expressed genes was performed. The top enriched biological processes included an inflammatory immune response, defense response and the pathways included the SODD
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Based on our finding that TFA modulates
2022-04-11
Based on our finding that TFA modulates GlyR function and reports that TFA-bound Thioguanine can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Tipps et al., 2010). No
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Introduction Histamine was generally accepted
2022-04-11
Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activiti
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The need for an inflammatory risk profile was recently
2022-04-11
The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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Regulation of Gja involves a member
2022-04-09
Regulation of Gja4 involves a member of the wingless-type MMTV integration site family, WNT4. Mice deficient in Wnt4 had reduced (30%) expression of GJA1 compared to WT mice [40]. It is thought that WNT signaling regulates GJA1 expression and GJIC in granulosa triclabendazole receptor by modulating
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The first GSM was identified from the discovery of
2022-04-09
The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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5-Azacytidine synthesis The conversion of lactose to GOS by
2022-04-09
The conversion of lactose to GOS by β-gal involves the same transglycosylation mechanism used by most glycoside hydrolases (GHs). This mechanism (Fig. 1) involves an enzyme-bound intermediate and consists of two processes: glycosylation and deglycosylation (Adlercreutz, 2017). The glycosylation proc
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