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br Cholecystokinin CCK CCK is secreted by enteroendocrine I
2021-12-03
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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ATP is essential for maintaining the ionic
2021-12-02
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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This work was supported by the
2021-12-02
This work was supported by the National Natural Science Foundation of China (Grants 81471101 and 81870852), the Natural Science Foundation of Jiangsu Province (Grant BK20181146), the Natural Science Foundation of the Jiangsu Higher Education Institutions of China (Grants 18KJA320007 and 17KJB320018)
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Studies regarding secretase nowadays aim
2021-12-02
Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran
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Since we were able to reach low micromolar
2021-12-02
Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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br Hydroxyfarnesyl diphosphate was synthesised in three step
2021-12-02
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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Acknowledgments br Introduction Stress plays a key
2021-12-02
Acknowledgments Introduction Stress plays a key role in the etiology and/or exacerbation of major depressive disorder characterized by loss of energy, feelings of hopelessness and anhedonia [1]. Ample evidence clearly suggests that endocannabinoids (eCBs) participate in stress-associated neurona
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br Results br Discussion Impaired BBB functions evoke vasoge
2021-12-02
Results Discussion Impaired BBB functions evoke vasogenic edema, which elevates intracranial pressure and leads to a life-threatening condition (Sperk, 1994, Unterberg et al., 2004, Simard et al., 2007). In addition, vasogenic edema formation results in the worsen consequence contributing to p
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In an attempt to further optimize
2021-12-02
In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou
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br Cellular directionality To obtain a comprehensive
2021-12-02
Cellular directionality To obtain a comprehensive understanding of cell migration, it is essential to understand how cues from the cell’s external environment are relayed to the ddhC cytoskeleton, so the cell can migrate towards the cue; a process herein referred to as cellular directionality. U
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GW was also the starting point for a study
2021-12-02
GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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Finally the formation of a regular network of fusion
2021-12-02
Finally, the formation of a regular network of fusion glycoproteins in their post-fusion state is not exclusive of vesiculovirus G. More or less regular networks have been also observed with other class III fusion glycoproteins such as pseudorabies gB [85] and several class II fusion glycoproteins [
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Though regulation of ghrelin interaction with GHSR has not b
2021-12-01
Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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br FXR expression in normal intestine and
2021-12-01
FXR Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant protein in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory
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In addition to the type of food consumed also the
2021-12-01
In addition to the type of food consumed, also the effect of calorie restriction (CR), i.e. an intermittent fasting and re-feeding cycles with concomitant fluctuations in the level of glucose and insulin, can affect the course of IBS through the modulation of the BA homeostasis. This type of nutriti
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