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On the other hand the single stranded RNA flavivirus hepatit
2021-11-11

On the other hand, the single-stranded RNA flavivirus hepatitis C virus (HCV), causes type C hepatitis, which often leads to liver cirrhosis, hepatic failure and hepatocellular carcinoma. Its genome of about 9.6kb encodes the structural proteins C, E1, E2, and the nonstructural proteins NS2, NS3, NS
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To further investigate the possible interaction of L with sG
2021-11-10

To further investigate the possible interaction of L1 with β1-sGC, a protein-ligand docking experiment was performed. Calculations were carried out with the program GOLD (version 5.2) [18], [34] and performed with the chemPLP scoring function [19], [34]. The ten lowest energy solutions presented a r
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Erastin br Conclusion In this report we describe
2021-11-10

Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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The importance of FXR FGF signaling in
2021-11-10

The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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A high throughput screening campaign of the
2021-11-10

A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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The post translational modification O GlcNAcylation is
2021-11-10

The post-translational modification O-GlcNAcylation is also dependent upon glucose fluctuations. O-GlcNAcylation has been linked to insulin resistance and glucose toxicity in diabetes and its comorbidities [11]. O-GlcNAcylation is a dynamic modification tightly regulated by the nutritional sensor UD
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Indeed our immunohistochemical analysis of skin tissue sampl
2021-11-10

Indeed, our immunohistochemical analysis of skin tissue samples without any pathology confirmed the expression of MR and GR. Extending earlier findings in rats (Shaqura et al., 2016a, Shaqura et al., 2016b), we demonstrate here that MR mainly colocalize with the nociceptive neuronal marker CGRP sugg
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Our results revealed that when subjected to intravenous gluc
2021-11-10

Our results revealed that when subjected to intravenous glucose tolerance tests, the RIP-Gcgr mice showed enhanced glucose tolerance and increased beta cell function, which is in agreement with the findings of Gelling et al. [6]. However, we also show that there is a reduced responsiveness of the be
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br FXR expression in normal intestine
2021-11-10

FXR A-443654 in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 200
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In a follow up study the same research group
2021-11-10

In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c
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Glucose induced nuclear translocation of several enzymes
2021-11-10

Glucose-induced nuclear translocation of several enzymes, including GK, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), muscle GS, aldolase, lactate dehydrogenase (LDH) and phosphoglycerate kinase (PGK) is a well-known phenomenon. Additional functions have been proposed for these enzymes in the nu
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FBP ALDOA complex is located on both
2021-11-10

FBP2-ALDOA complex is located on both sides of Z-line in striated muscles (Rakus et al., 2003a; Gizak et al., 2003) and its stability is regulated by calcium ions (Mamczur et al., 2005; Rakus et al., 2013) (Fig. 3). An increasing titre of [Ca2+] which occurs during muscle contraction stimulates diss
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Andexanet alfa works as a decoy for the FXa inhibitor
2021-11-10

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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As part of our discovery efforts searching
2021-11-09

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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SB 242084 receptor The results of our study
2021-11-09

The results of our study indicate the general importance of the gp120 V3 loop SB 242084 receptor patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to g
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