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One PKC target that controls cortical actin
2021-10-27

One PKC target that controls cortical PMX 205 structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC releases MARCKS f
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Adipocytes play diverse roles in energy homeostasis by
2021-10-27

Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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Bile acids are the end products of
2021-10-26

Bile acids are the end products of cholesterol catabolism and have also been considered as hepatomitogens. Recently, Yap has been shown to be activated by the mevalonate pathway, which is essential for the biosynthesis of isoprenoids and downstream cholesterol and bile acids (Sorrentino et al., 2014
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Starting from commercially available dioxaspiro decan ol was
2021-10-26

Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an TUG 891 catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼3/2) was obtai
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Methods br Results br Discussion The current
2021-10-26

Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n
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Consistent with these observations impaired transduction of
2021-10-26

Consistent with these observations, impaired transduction of the glutamate signal by NMDARs (i.e., NMDA receptor hypofunction [NRH]) by parvalbumin-containing GABAergic inhibitory interneurons is implicated in mediating social deficits, a domain of psychopathology responsible for poor functional out
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Trypanosomatid GLO enzymes are monomeric and
2021-10-26

Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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Interestingly when glucose is deleted in PCa cells GLUT is
2021-10-26

Interestingly, when glucose is deleted in PCa cells, GLUT1 is increased. Also, AR is almost entirely located in the nucleus, correlating with the increment in GLUT1 levels. These results are in agreement with those reported by Vaz et al. [16], They described an increase in GLUT1 after DHT stimulatio
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In the GLUT family glucose transporter
2021-10-26

In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis
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The expression of GLUT receptors throughout the body could b
2021-10-26

The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as we
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The rapid actions of glucocorticoids range from
2021-10-26

The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune Ro 61-8048 australia [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapi
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Different from stable transfection transient expression
2021-10-26

Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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Most of the above mechanisms
2021-10-26

Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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We next determined the selectivity
2021-10-25

We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Dehydroepiandrosterone receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affini
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Next we were interested in replacing the ketobenzimidazole f
2021-10-25

Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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