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br Results and discussion br Conclusion In
2021-10-22
Results and discussion Conclusion In summary, starting from our previous lead sr9009 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good agoni
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Restless running behavior was first
2021-10-22
‘Restless running behavior’ was first described in mice after administration of 30mg/kg i.p. ALX-5407 and was thought to be due to an augmentation of NMDA-induced dopamine activity [27]. The motor impairments caused by ALX-5407 were confirmed by Perry et al. [10] and extended to another sarcosine-de
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Experiments conducted on the human parasite Leishmania major
2021-10-22
Experiments conducted on the human parasite Leishmania major has shown that specific parasitic antigens are involved in steering the immune responses to “protective” as opposed to “disease” state (Reiner et al., 1993; Reiner and Locksley, 1995; and Sjölander et al., 1998) and that antigenic composit
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br Conflict of interest br Funding br Acknowledgements
2021-10-22
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino 9516 derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediated trans
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br Materials and Methods br Results br Discussion A model
2021-10-22
Materials and Methods Results Discussion A model of seizure and excitotoxicity induced by neonatal MSG administration was described recently (19) in which extracellular glutamate increased after the first and second MSG administrations were observed, the greatest increase seen following the
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br Conclusions We have shown that despite the
2021-10-22
Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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br Introduction Calorie restriction CR in the absence of mal
2021-10-22
Introduction Calorie restriction (CR), in the absence of malnutrition, has beneficial effects on Ion Channel Compound Library function, including reducing the incidence of age-related neurodegenerative disease (Gräff et al., 2013), eliciting anti-depressant behavior (Lutter et al., 2008) and impr
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Signaling pathways such as BMP FGF and WNT are
2021-10-21
Signaling pathways such as BMP, FGF, and WNT are strongly involved in the process of endochondral ossification and Meckel's cartilage development [20]. Interestingly, absence of BMP antagonist, Noggin, in Meckel's cartilage, resulted in a phenotype, very similar to that of Setdb1 CKO [16]. To examin
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Noticeably aminopyrimidine analogs are the
2021-10-21
Noticeably, aminopyrimidine analogs are the most widely published H4R antagonists and it was Bayer who first disclosed two series of 2-aminopyrimidine compounds possessing significant H4R functional activity. Subsequently, further 2-aminopyrimidine H4R antagonists were published by Pfizer (ZPL-38937
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The therapeutic potential of acetate has
2021-10-21
The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi
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Resolving the molecular details of
2021-10-21
Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar
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br Regulation of plasma ghrelin concentration
2021-10-21
Regulation of plasma ghrelin concentration As described above, ghrelin is primarily produced in the stomach and secreted into the blood stream. Plasma ghrelin does not significantly differ between chronic heart failure (CHF) patients and controls, although plasma ghrelin level is significantly hi
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br Acknowledgments br Introduction When human red blood cell
2021-10-21
Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact cyclic amp function suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-dependen
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In general substrates that undergo regulated intramembrane p
2021-10-21
In general substrates that undergo regulated intramembrane proteolysis are initially cleaved in the extracellular domain by sheddases such as TACE (TNFα converting enzyme) or ADAM (a disintegrin and metalloproteinase domain)/α-secretase, or by aspartyl proteases, such as BACE/β-secretase, before cle
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The focused set of additional pyrazole analogs allowed
2021-10-21
The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro
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