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As early as glucagon was shown to
2021-12-30
As early as 1957, glucagon was shown to increase bay 11 receptor expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27].
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br Introduction The glucagon receptor
2021-12-30
Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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There are additional implications of
2021-12-29
There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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Due to the presence of all FGFRs in
2021-12-29
Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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67 8 mg Remarkably most of these molecules are also quite
2021-12-29
Remarkably, most of these molecules are also quite effective in interfering with the proliferation of the drug-resistant cancer cell lines, with IC50 values ranging from 0.59 to 2.93 μM against MCF-7/ADR cells, and from 0.160 to 1.17 μM against NSCLC-resistant H1975 cells. Among these molecules, com
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Nonetheless several questions remain to be answered about FA
2021-12-29
Nonetheless, several questions remain to be answered about FAAH inhibition to address cannabis use disorder. The trial was of short duration (4 weeks), whereas most clinical trials in this field have been for 8–12 weeks., , , Although motivational deficits are commonly present in cannabis users and
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Nonetheless several questions remain to be answered about FA
2021-12-29
Nonetheless, several questions remain to be answered about FAAH inhibition to address cannabis use disorder. The trial was of short duration (4 weeks), whereas most clinical trials in this field have been for 8–12 weeks., , , Although motivational deficits are commonly present in cannabis users and
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Certainly the immune relevance of Hippo
2021-12-29
Certainly, the immune relevance of Hippo becomes more complicated and divergent in the vertebrates than in Drosophila. In terms of inflammation of mammalians, the stories are diversified (Fig. 2). Previously, MST1/2 has been well characterized not only as a controller of lymphocytes adhesion and mi
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The medicinal properties of guanidine derivatives are also
2021-12-29
The medicinal properties of guanidine derivatives are also of great interest due to their diverse anti-microbial, anti-inflammatory, anti-viral, and anti-cancer, activities (C and D). Guanidine-containing drugs, such as -iodobenzylguanidine and methylglyoxal bis(guanylhydrazone), were shown several
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ANT located in the IMM mediates the
2021-12-29
ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions
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br Results and discussion br Conclusions A
2021-12-29
Results and discussion Conclusions A series of novel HDAC inhibitors comprising the thioquinazolinone were designed and synthesized. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines. Then we chose compounds 7a, 4i, 4o, and 4p to fu
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In summary P P macrocyclization proved to
2021-12-29
In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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It has been reported that expression of murine haspin is
2021-12-29
It has been reported that expression of murine haspin is found only in post-meiotic spermatids and that overexpression of murine haspin in HEK-293 cells leads to reduced cell proliferation. Therefore, it was suggested that haspin functions to bring about casin arrest in haploid germ cells (Tanaka e
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Under most circumstances NO is a potent endogenous vasodilat
2021-12-29
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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Racemic protein crystallography has been proven to be a powe
2021-12-29
Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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