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In summary we have discovered the first examples of
2021-11-25

In summary, we have discovered the first examples of movement of Asp189 upon binding to fXa inhibitors. A series of novel and potent fXa inhibitors with a phenyltriazolinone P moiety were identified. Although the general binding mode compared to our previously-reported fXa inhibitors was maintained,
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Accumulating evidence suggests that the NGF
2021-11-25

Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, somatostatin agonist derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF
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The mechanistic basis of a PAE induced reduction in HDC
2021-11-25

The mechanistic basis of a PAE-induced reduction in HDC isoform expression is unclear at present. These reductions may be a consequence of reduced histaminergic innervation of PAE-affected brain regions. Given that these three brain regions are anatomically more distant from the ventral hypothalamus
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Preadipocytes are capable of differentiating into
2021-11-25

Preadipocytes are capable of differentiating into lipid-laden mature adipocytes. Lipid droplets are a prominent morphological feature of mature adipocytes, which is accumulated and maintained during adipocytes differentiation [26]. In this study, rHhip treatment increased lipid accumulation, as well
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br Materials and methods br
2021-11-24

Materials and methods Results Discussion To understand the molecular basis for how ghrelin secretion is regulated at the cellular level, we identified the full repertoire of 7TM receptors and G proteins in gastric ghrelin Maprotiline HCl synthesis and functionally characterized the majorit
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The advent of next generation sequencing NGS has shown that
2021-11-24

The advent of next-generation sequencing (NGS) has shown that considerable variation in human genome is still undiscovered and therefore a considerable number of rare variations that are related to disease susceptibility may still be unknown. NGS has allowed to strengthen the association between los
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To maintain low Glu concentrations in
2021-11-24

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino C-type natriuretic peptide (1-22) (human, rat, swine) australia is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in
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Previously we have shown that ghrelin and
2021-11-24

Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo
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Polymerisation of HbS initiates the clinical complications o
2021-11-24

Polymerisation of HbS initiates the clinical complications of SCD (Bunn and Forget, 1986). The resulting sequelae are multiple and diverse, and their individual impact on pathogenesis is difficult to elucidate. Early changes include altered red cell membrane permeability (Gibson and Ellory, 2002, Le
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br Materials and methods Manganese chloride MnCl H
2021-11-24

Materials and methods Manganese chloride (MnCl2·4H2O), glutamate, glutamine, Lucifer Yellow, polyclonal anti-GFAP and MTT assay kits were purchased from Sigma Chemical Co. (St. Louis, MO). Dulbecco's Modified Eagle's Medium-F12 (DMEM-F12) with Earle's salts, foetal bovine serum, penicillin, and s
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The effects of FFAR and FFAR activation in
2021-11-24

The effects of FFAR1 and FFAR2 activation in different tissues have been reported in several species (Hara et al., 2014). Herein, we report the first evidence for differential expression of FFAR1 and FFAR2 during the peripartal period in the liver of dairy cows that differ in liver metabolism, based
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In early a collaborative effort
2021-11-24

In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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After the successful development of molecular targeted drugs
2021-11-24

After the successful development of molecular targeted drugs in lung adenocarcinoma, substantial efforts have been made to provide similar targeted drugs in lung squamous-cell carcinoma. Because FGFR gene alteration is the most frequent occurrence in squamous-cell carcinoma, targeted therapies for F
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Nutlin-3a br Material and methods br Acknowledgements and
2021-11-24

Material and methods Acknowledgements and funding The authors thank Katharina Elsässer for technical support and Emma Esser for careful editing of the manuscript. We also thank Marcus Conrad for providing Liproxstatin-1 and advisory comments and discussion on the manuscript. This work was part
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PR957 The Ala to Leu substitution would reduce
2021-11-24

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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