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The compounds described in this paper were prepared using
2022-01-29

The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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br Materials and methods br Results br Discussion Since
2022-01-29

Materials and methods Results Discussion Since 1990s, solving structures for most DNA glycosylases by X-ray crystallography significantly advanced mechanistic understanding of the catalytic activity and substrate specificity of this important class of DNA repair enzymes. However, static str
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In this study we find
2022-01-29

In this study, we find that DH-CBD induces analgesic effects on inflammatory but not acute pain and the FPS-ZM1 level of spinal α1 GlyRs increased after CFA paw injection. These results suggest that GlyR α1 is only involved in chronic pain. A possible explanation is that once the expression of α1 G
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The development of immobilization techniques for
2022-01-29

The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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It is increasingly argued that
2022-01-29

It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit GSK256066 of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC-mediated repressi
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br Introduction The glucagon receptor GCGR is a G protein
2022-01-29

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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To improve the preferential GalR binding we synthesized M wh
2022-01-29

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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Recently Bristol Myers Squibb and Merck reported
2022-01-28

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic bifonazole derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists
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Some studies using RNAi have
2022-01-28

Some studies using RNAi have recently been invalidated by CRISPR/Cas9 [25] due to significant off-target effects of RNAi [26]. In this study, we have used both RNAi and CRISPR/Cas9 techniques and have observed consistent and similar phenotypes thus; knockdown or knockout of PATZ1 resulted in reducti
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The RAS RAF MEK ERK pathway is a
2022-01-28

The RAS/RAF/MEK/ERK pathway is a central controller of cell proliferation and survival and, consequently, alterations to some of its components lead to hyperactivation of the pathway, an event related to numerous types of cancer [172]. High rates of alterations to this pathway are found in leukemia,
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br Introduction Hepatitis B virus
2022-01-28

Introduction Hepatitis B virus (HBV) infects about 2 billion people worldwide and is a leading cause of liver disease including liver fibrosis, cirrhosis and hepatocellular carcinoma (Trepo et al., 2014). Most current HBV therapies are based on nucleos(t)ide analogs and pegylated interferon alpha
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Recently it was found that
2022-01-28

Recently, it was found that hypoxia results in the phosphorylation of β-catenin at Y654 in a Src-dependent manner (Xi et al., 2013). All β-catenin phosphorylated at this residue was found complexed with Hif1α and it was demonstrated that this β-catenin phosphorylation was required for Src to promote
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Although some PAHs that are human carcinogens have
2022-01-28

Although some PAHs that are human carcinogens have been found in the sugarcane soot (Zamperlini et al., 1997), there are no data about cancer incidence among sugarcane workers. To the best of our knowledge, this is the first report of an evaluation of internal exposure, comparing the harvesting (whe
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br Conclusion GST expression was detected
2022-01-28

Conclusion GST expression was detected in the Hemicornea construct and the commonly used animal cornea models at both the protein and functional levels. The results are summarized in Table 1. However, the construct exhibited lower levels of activity of GST, a marker of phase II enzymatic activity
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Additionally OsGly I overexpressing transgenic rice
2022-01-28

Additionally, OsGly I-overexpressing transgenic rice plants had higher grain yields than WT (Table 2). Although there were no significant differences in the number of effective panicles per plant, panicle length, grain numbers per panicle, or 1000-grain weight between WT and transgenic plants, the s
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