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Deferasirox The calculations for the R substrate showed that
2022-01-27
The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn Deferasirox is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged role
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In Locusta migratoria a worldwide agricultural
2022-01-27
In Locusta migratoria, a worldwide agricultural pest, we previously identified 51 CPRs containing eight endocuticle structural glycoproteins, which are homologs of SgAbd-1, SgAbd-2, SgAbd-3, SgAbd-4, SgAbd-5, SgAbd-6, SgAbd-8, and SgAbd-9 in the adult desert locust, Schistocerca gregaria [17,26]. Al
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GlyRs are members of the superfamily
2022-01-27
GlyRs are members of the superfamily of Cys-loop receptors (CLRs) [3]. They form postsynaptic pentameric receptor complexes of α1 and β subunits anchored via the scaffolding protein gephyrin [4]. GlyRs are composed of several domains with the large N-terminal extracellular domain (ECD) important for
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br Funding This work was supported by the Deutsche
2022-01-27
Funding This work was supported by the Deutsche Forschungsgemeinschaft (SFB766 and GRK1708). Conflict of interest Acknowledgements Introduction Hepatitis C virus (HCV) infection is a global problem affecting about 3% of the world’s population [1], [2]. Mother-to-child transmission of HC
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br SMO antagonists pitfalls and limitations The first Hh
2022-01-26
SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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br Although D reconstruction of an invertebrate gap junction
2022-01-26
Although 3D reconstruction of an invertebrate gap junction channel from native tissue of crayfish was reported in 1991, the negative-staining EM imaging was limited to low-resolution structural analysis [39]. The oligomeric number of innexin channels was believed to be the same as that in connexin
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The focused set of cyclopentapyrazoles produced six compound
2022-01-26
The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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The galactosidase from Aspergillus oryzae is
2022-01-26
The β-galactosidase from Aspergillus oryzae is a monomeric enzyme of 113 kDa [58] that has been widely used in GOS synthesis [49,53,[59], [60], [61]], exhibiting a high activity of lactose transgalactosylation [62]. Different immobilization methods have been used for the synthesis of lactose-derived
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Another small compound targeting IBAT has
2022-01-26
Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause
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Compounds were tested for GPR activity in a functional
2022-01-26
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO kd025 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity relat
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Tail group SAR of the imidazole derived analogs
2022-01-26
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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br Introduction Adenosine triphosphate ATP is an organic
2022-01-26
Introduction Adenosine-5′-triphosphate (ATP) is an organic molecule (nucleoside triphosphate) which consists of adenine, ribose, and three phosphoric SB273005 residues. ATP serves as a temporary carrier of energy in all living cells, so it is a common substance in any organism. In the cells, new
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Overall this study provides compelling evidence that overexp
2022-01-26
Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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In summary through medicinal chemistry design and
2022-01-26
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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Historically a role for the prefrontal cortex
2022-01-25
Historically, a role for the prefrontal cortex in spatial working memory has been repeatedly claimed (for review, see Kolb, 1984). Older studies using traditional, non-fibre-sparing lesions (e.g. aspiration lesions) often resulted in spatial alternation deficits. In contrast, more recent studies emp
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