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As a possible back up to
2021-09-03
As a possible back-up to Sch 503034 (), we explored inhibitors that contained alternative electrophiles to ketoamides. Boronic acids have been extensively investigated as possible electrophiles that could react with nucleophilic serine in the context of developing inhibitors of thrombin receptor and
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In this study we demonstrated that while Cu
2021-09-03
In this study, we demonstrated that while Cu(I) does not affect LPS induced iNOS ABT737 it inhibits NO release from microglia. Cu(I)-induced GSNOR inhibition and GSNO depletion is more in line with alternative (non-inflammatory) polarization. These results extend our previous findings that Cu(I) eli
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The GPR gene was included in
2021-09-02
The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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However even if immunological tests with
2021-09-02
However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21 p
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Cortisol targets many organs and tissues and has
2021-09-02
Cortisol targets many organs and tissues and has certain effects on metabolism, including promoting glycolysis. It can cross the blood Camptothecin barrier and act centrally to regulate HPA axis activity by activating negative feedback mechanisms effectively, cortisol inhibits its own production (F
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Thus this work aims to evaluate the effect of tannic
2021-09-02
Thus, this work aims to evaluate the effect of tannic gw501516 on β-galactosidase activity, by observing the variations in the molecular interaction kinetic parameters ( and ). Besides, these data were correlated with the modifications that the tannin caused to the enzyme’s secondary structure (CD),
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Introduction Risk factors for colorectal
2021-09-02
Introduction Risk factors for colorectal cancer (CRC) include high-fat diets, sedentary lifestyles, obesity, diabetes, and elevated serum levels of toxic bile acids (BAs) (de Aguiar Vallim et al., 2013, Degirolamo et al., 2011, Downes and Liddle, 2008, Font-Burgada et al., 2016, Kuipers et al., 201
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One effective approach to fine tuning the lipophilicity
2021-09-02
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Octreotide acetate synthesis scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 an
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br Materials and methods br Results
2021-09-02
Materials and methods Results and discussion In order to identify genes required for photoautotrophic growth, we screened a random insertion mutant library of Synechocystis 6803 and obtained many mutants with impaired photoautotrophic growth. About 6000 random insertion colonies of the mutant
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Conformational analysis provides further insight
2021-09-02
Conformational analysis provides further insight into the SAR trends apparent in . Acyclic precursors – are 25–50-fold less active than their macrocyclic counterparts – against Pyk2. The global minima for – are conformations in which the –NHCH– linker between the pyrimidine and pyridine rings is sta
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dibromide synthesis br Materials and methods br Results and
2021-09-02
Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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The majority of APC C
2021-09-02
The majority of APC/C subunits form a giant scaffold, which was originally named the arc lamp, based on its shape when viewing APC/C from one side (Figure 1 and Box 1) [24]. The scaffold consists of two modules: the TPR lobe resembles the curved post and lamp, and the platform resembles the Cy5 male
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Our data also showed that D dopamine receptor was
2021-09-02
Our data also showed that D2 dopamine receptor was down-regulated in the hippocampus, NAc and striatum of F1-MEP animals, which was only significant in the hippocampus. Both agonists and antagonists of D2 dopamine receptor are able to decrease heroin self-administration (Hemby et al., 1996; Rowlett
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For the SAR optimization of the right hand side
2021-09-01
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic what can not moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by conden
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br Materials and methods br Results br Discussion In
2021-09-01
Materials and methods Results Discussion In general, CI symptoms are often visible only after the chilled products have been removed from coolstore to a warmer temperature (Schirra and Cohen, 1999). However, in the present work, 'satsuma’ mandarin fruit stored at 2°C showed chilling symptom
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