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The PI K PTEN Akt mTORC GSK pathway also plays
2022-03-21
The PI3K/PTEN/Akt/mTORC1/GSK-3 pathway also plays key roles in metabolism, obesity, diabetes and cardiovascular diseases (, , , , ). Sometimes such clinical problems such as diabetes, obesity and metabolic disorders are interlinked with cancer. Clearly further elucidation of the roles of GSK-3 could
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In addition to the role of
2022-03-21
In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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1,2-Dimyristoyl-sn-glycerol Tail group SAR of the imidazole
2022-03-21
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Genetic rescue of GluR A dependent spatial working
2022-03-21
Genetic rescue of GluR-A-dependent spatial working memory Spatial working memory performance in GluR-A−/− mice can be restored by the forebrain-specific histamine-1 receptor antagonist of GluR-A subunits labeled with green-fluorescent protein (GFP) on an otherwise GluR-A knockout background (Schm
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Until now various reports have demonstrated
2022-03-21
Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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As many of the above studies highlight several
2022-03-21
As many of the above studies highlight, several decades of research on Cx43 has revealed that many of these functional roles are attributed to the C-terminal domain (CT) of this protein which cannot be explained by the formation and existence of intercellular channels. Recent findings on the existen
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br Activators Many compounds are known to
2022-03-21
Activators Many compounds are known to influence the activity of Ca2+-activated K+ channels, and since hIK1 was cloned more insight has been gained on compounds that have the capacity to increase channel activity. Activation by divalent metal cations has been investigated, with Ca2+, Pb2+, Cd2+,
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Riluzole br GSMs Secretase cleavage of APP generates a numbe
2022-03-21
GSMs γ-Secretase cleavage of APP generates a number of Aβ peptides [32], [137]. In most cells Aβ1–37, 38, 39, and 42 are produced at low levels (typically each represents 5–20% of total Aβ detected) and the major species generated is Aβ1–40 (typically over 50% of total Aβ). Other Aβ peptides can
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Introduction Since the development of the first radioimmunoa
2022-03-21
Introduction Since the development of the first radioimmunoassay (RIA) to measure hormone levels in the late 1950s, for which Rosalyn Sussman Yalow was awarded the Nobel Prize for Medicine in 1977 (the second woman ever receiving it), the use of SNS-314 Mesylate receptor in molecular research has
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br Medium to long chain fatty acids Medium to long
2022-03-21
Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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All of the abovementioned effects
2022-03-18
All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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br Introduction Isoprenoid structures play an essential role
2022-03-18
Introduction Isoprenoid structures play an essential role in biology and over 30,000 natural products of this class are known (Greenhagen et al., 2003). Like other animals, insects require these compounds for many disparate processes, including electron transport (e.g., ubiquinones), protein glyc
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br Experimental br Results br Discussion In this
2022-03-18
Experimental Results Discussion In this study, we performed molecular docking analysis and in vitro studies to determine whether genistein binds to HIF-1α in BC TCS JNK 6o mg and identify the residues involved in this interaction. We found that some functional groups (residues) mimic the bi
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In our previous study we designed and synthesized compounds
2022-03-18
In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic xanthine oxidase (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro a
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In summary we have designed and explored synthetic routes to
2022-03-18
In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com
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