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Fatty acids have been repeatedly shown
2022-07-06
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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Active compounds and were further tested and EC and
2022-07-06
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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Glucagon regulates the transition from hepatic
2022-07-06
Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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Our results revealed that when subjected to intravenous gluc
2022-07-06
Our results revealed that when subjected to intravenous glucose tolerance tests, the RIP-Gcgr mice showed enhanced glucose tolerance and increased beta cell function, which is in agreement with the findings of Gelling et al. [6]. However, we also show that there is a reduced responsiveness of the be
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The eradication of agonist activity in compound was also con
2022-07-06
The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Fmoc-Tyr(tBu)-OH mg as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antag
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The identity of the K transport pathway activated by
2022-07-06
The identity of the K+ transport pathway activated by NEM remains unclear. The pathway does not require the presence of Gardos channel KCNN4 or K–Cl cotransporters KCC3 and KCC1, but like these pathways is sensitive to the presence of hemoglobin S or other sickling hemoglobins. Although partially se
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The deduced amino acid sequences of all scIPPSs display
2022-07-05
The deduced amino R406 free base sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid residue)
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According to the implication of
2022-07-05
According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst
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Although it is well documented that FAAH
2022-07-05
Although it is well documented that FAAH substrates can elicit analgesic effects [for review see [47,48] and that systemic poly I:C administration induces mechanical allodynia in rats [14], to our knowledge this is the first study to demonstrate that enhancing FAAH substrate levels can modulate TLR3
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In addition the interplay of membrane curvature induced tens
2022-07-05
In addition the interplay of membrane curvature induced tension at the fusion pore and Fmoc-Asp-OAll sale induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity warrant fu
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This study appears to provide
2022-07-05
This study appears to provide an additional example, albeit an unanticipated one, of the importance of renal ETB receptor function in the normal control of blood pressure and salt and water homeostasis. ETB receptor-deficient rats, collecting duct-specific ETB receptor knockout mice, and rats chroni
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A new series of pyrimidones with C and C
2022-07-05
A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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In humans polymorphisms in the lengths of GT sequences from
2022-07-04
In humans, polymorphisms in the lengths of GT sequences (from 11 to 40) within the HMOX1 promoter impact the magnitude of HO-1 expression profiles. Long GT repeats code for less stable (Z-conformational) DNA with blunted transcriptional activity resulting in lower resting and stimulated HO-1 protein
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Cells undergoing EMT display a downregulation of E
2022-07-04
Cells undergoing EMT display a downregulation of E-cadherin and dissociation of their junctional complexes that associates cell-cell contacts with the nisoldipine sale cytoskeleton, known as the adherens junction (Berx and van Roy, 2009, Birchmeier and Behrens, 1994). Adherens junctions are special
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Retapamulin br Materials and methods br Results br Discussio
2022-07-04
Materials and methods Results Discussion GSK-3 overexpression diminishes neurogenesis (Fuster-Matanzo et al., 2013, Kondratiuk et al., 2013, Sirerol-Piquer et al., 2011), while the inhibition of GSK-3 with lithium or valproate enhances neurogenesis, as measured by cell proliferation, the nu
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