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It was previously proposed that glucagon
2021-12-06

It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the ABT via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the liver but not
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br Introduction Connexins are transmembrane proteins that al
2021-12-06

Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent Flavin adenine dinucleotide receptor via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nu
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In order to address the
2021-12-06

In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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We have previously designed an azobenzene
2021-12-04

We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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rifampicin Herein we describe the design and optimization of
2021-12-04

Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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According to the implication of the endocannabinoid system i
2021-12-04

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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Regulation of gene expression in mammalian cells is
2021-12-04

Regulation of gene expression in mammalian cells is governed by the epigenetic machinery, which includes several distinctive yet entangled branches. DNA and histone modifying enzymes, non-coding regulatory RNAs, and ATPase-dependent chromatin remodeling proteins all contribute to the dynamic alterat
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The H R antagonist cimetidine Tagamet
2021-12-04

The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Importantly the regulation of the Hippo pathway by metabolic
2021-12-04

Importantly, the regulation of the Hippo pathway by metabolic networks, such as by glycolysis39, 40, hexosamine biosynthesis41, 42, and mevalonate synthesis43, 44, as well as by nutrient-sensing pathways including AMP-activated protein kinase (AMPK) 40, 45, 46 and mTOR 47, 48, 49, 50, was recently d
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Compound was synthesized starting from
2021-12-04

Compound was synthesized starting from α-cyclopropyl glycine (). After protection of the free amine via methyl carbamate and esterification to the methyl ester, the pyrrolidine core was furnished by condensation with methyl acrylate under basic conditions. Double deprotonation of the pyrrolidine fol
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SB273005 synthesis Reports described a range of synthetic GP
2021-12-03

Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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FXa is a vitamin K dependent serine protease consisting of
2021-12-03

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 ML385 and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The active s
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The cases of the Berlin and London patients also highlight
2021-12-03

The cases of the Berlin and London patients also highlight our limits to defining an HIV cure. No signs of the virus have been found in numerous assays with multiple samples from diverse tissues that Timothy Brown has generously contributed to advance research over the past 12 years. In the case of
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br Discussion Our study found that of MSM from
2021-12-03

Discussion Our study found that 62.6% of MSM from Natal had been tested for HIV before. This rate was higher than the national average of 37% estimated for the general Sorafenib australia in 2011 and the 51.6% found by Brito et al. in MSM from 10 Brazilian cities in 2009. These rates are rather d
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Furthermore the identification of the
2021-12-03

Furthermore, the identification of the inhibitory effect of P. grandiflorum and ginseng extract on HDAC represents an effective workflow for gene expression similarity-based repositioning of nutraceuticals. Acknowledgments This research was supported by Basic Science Research Program through the
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