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PBI is an agonist of
2021-12-07
PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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There were significant differences in mRNA
2021-12-07
There were significant differences in mRNA expression levels observed for 7 out of 15 analyzed genes. This observation suggests, that selection of a reference/control group may influence interpretation of gene expression studies performed in liver pathologies. This study directly evidenced that anal
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X-NeuNAc br Introduction Prostate cancer is the most
2021-12-07
Introduction Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths in men in the United States, accounting for about 30,000 cancer deaths annually [1]. Epidemiological studies that show geographical variations in prostate cancer incidence and mortali
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br Dysregulation of glutamate transporter expression and fun
2021-12-07
Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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br Introduction Most organisms require glucose
2021-12-07
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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Up to now the research about the
2021-12-07
Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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Nevertheless in the brain we found that trehalose phosphoryl
2021-12-07
Nevertheless, in the brain, we found that trehalose phosphorylates AMPK, which is a metabolic sensor. AMPK is known to be transiently activated in muscle by acute exercise [21,22]. Bayod et al. also reported that AMPK was significantly activated in both the cerebral cortex and hippocampus in exerci
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br Material and methods br Results br Discussion
2021-12-07
Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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Growth hormone secretagogue receptor GHSR is a member
2021-12-07
Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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br Materials and methods br Results Unitary currents
2021-12-07
Materials and methods Results Unitary currents of Gardos Difopein sale were identified by their conductance value, inward rectification, voltage independence of open probability, kinetics and Ca2+-sensitivity, all features which have been described elsewhere [8], [13], [20], [23], [24], [25],
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With rare exceptions the biological role of secretase cleava
2021-12-06
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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The present in vitro experiments confirm previous suppositio
2021-12-06
The present in vitro experiments confirm previous suppositions (Ciosek, Gałecka, 2011, Izdebska, Ciosek, 2010) that Gal modulates AVP and OT release by acting at every level of the hypothalamo-neurohypophysial system. In fact, both 10−10 M and 10−8 M Gal diminished basal release of AVP and OT from t
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Recently Bristol Myers Squibb and Merck reported their GPR
2021-12-06
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic pp2 derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists with h
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Among the various epigenetic mechanisms involved in EwS path
2021-12-06
Among the various epigenetic mechanisms involved in EwS pathogenesis, we focused on the PRC enzyme EZH2, since it is a direct target of EWSR1-FLI1 and a critical mediator of malignant cell growth.24, 30 Our observation that the inhibition of EZH2 in GD2neg EwS mao inhibitors induces GD2 expression
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At baseline Hdc KO mice have alterations in the examined
2021-12-06
At baseline, Hdc-KO mice have alterations in the examined signaling cascades that resemble those seen in WT mice after RAMH challenge. Specifically, vascular disrupting agent of MSK1 at T581 and of rpS6 ad S235/236 are elevated in dMSNs to a similar extent after saline in KO mice and after RAMH cha
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