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Kartogenin br ABT aR aR methyl hexahydropyrrolo
2022-09-24

ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo
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br Acknowledgement The work was supported by
2022-09-24

6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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Assays can perform differently by genotype and under
2022-09-22

Assays can perform differently by Garcinol and under-quantification of HCV GTs has been seen with HCV assays [8], [9], [10], [11]. Under-quantification of GT4 has been reported in some early studies of the VERIS Assay [7], [12] where a bias greater than −0.5 log10IU/mL was seen. In two more recent
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Importantly each conformational state in
2022-09-22

Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon
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Also the decrease in adipocyte cAMP levels seen after an
2022-09-22

Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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The pharmacokinetics of was obtained
2022-09-22

The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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In addition http www apexbt com media
2022-09-21

In addition to genomics, transcriptomics and proteomics tools, metabolomics approaches are now used in order to optimize glycoprotein production in CHO cell lines. Recent advances in metabolite quantification have allowed identification of cellular phenotypes under specific experimental conditions (
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br Glycoengineering br The Omics
2022-09-21

Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO Acarbose synthesis for improved glycoprotein pr
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Introduction Glucose is the most important energy carrier
2022-09-21

Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula
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br Materials and methods br Results br Discussion Here
2022-09-21

Materials and methods Results Discussion Here, we investigated the inhibitory effects and associated mechanisms of phloroglucinol on α-glucosidase. Our results showed that phloroglucinol reversibly inhibited α-glucosidase in a dose-dependent manner (Fig. 1), with the double-reciprocal plot
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The bioconversion of inositol from glucose was anticipated n
2022-09-21

The bioconversion of inositol from glucose was anticipated nearly a century ago and later confirmed by isotope tracing methods [[22], [23]]. This biosynthesis of inositol involves three sequentially acting enzymes: Firstly, ATP-dependent glucokinase converts glucose to glucose-6-phosphate (G-6P) [[2
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br Conclusions We have shown that despite the development of
2022-09-21

Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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A significant contribution to the discovery of novel
2022-09-21

A significant contribution to the discovery of novel Hh inhibitors is given by natural compounds [11,17,22,31,32]. The first Hh inhibitor ever discovered has been Cyclopamine, a steroidal alkaloid isolated from plants of the Veratrum species [13,33]. Subsequently, many natural compounds belonging to
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The Notch cleavage efficiency of Aph aS containing complexes
2022-09-21

The Notch-cleavage efficiency of Aph1aS containing complexes was lower than that of Aph1aL γ-secretases, especially in combination with PS2, suggesting that Aph1aS is a determinant of low Notch-cleavage specificity, considering that the different subcellular localization of PS1 and PS2 didn't affec
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br Experimental br Results and
2022-09-21

Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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