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Further research should indeed focus on understanding the nu
2021-09-13
Further research should indeed focus on understanding the nutritional value of food and its effect on metabolism, overall activation of metabolic NRs network. Moreover, given the prominent role of microbiota in the modulation of the FXR signalling (Degirolamo et al., 2014), there is enough impetus t
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Studies of human and mouse GPR
2021-09-13
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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br Material and methods br Acknowledgements and funding
2021-09-13
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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br PEPCK This enzyme decarboxylates and
2021-09-13
PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Conflicts of interest br Significance p is
2021-09-11
Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig
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As disclosed in our preceding paper medicinal chemistry SAR
2021-09-11
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, 69 6 lacks an essentia
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AFB Fapy dG has been long recognized as a
2021-09-11
AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by MAPK Inhibitor Library mg excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB
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br Parkinson disease Idiopathic PD is a
2021-09-11
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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Under most circumstances NO is a potent endogenous
2021-09-11
Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response
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br Introduction Depression is a prevalent and disabling psyc
2021-09-11
Introduction Depression is a prevalent and disabling psychiatric illness that affects millions of individuals worldwide, resulting in enormous personal suffering and public health costs [1]. Traditional antidepressants such as monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake
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To get a broader view of the interplay
2021-09-11
To get a broader view of the interplay between glycolysis and Hippo signaling, we tested the involvement of YAP1 in the regulation of C-MYC and GLUT1 expression. We were able to detect a YAP1-TEAD1 interaction in the nuclear fraction of Jurkat angiotensin receptor blocker and confirm the inhibition
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Analysis of the GHSR screening data for inactive
2021-09-11
Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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Cys loop GABA receptors are well studied
2021-09-10
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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potassium channel blockers Further our data demonstrate a ro
2021-09-10
Further, our data demonstrate a role for mitochondrial AIF in oxidative cell death induced by RSL3. We found that AIF knockdown using siRNA completely protected the potassium channel blockers against RSL3 induced oxidative stress. Similar to other pathways of caspase-independent programmed cell dea
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Here we examine the impact of hypoxia on
2021-09-10
Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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