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br Conclusion In this report we describe the synthesis and
2022-08-05
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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digital etiquette To characterize the basic functions of GPR
2022-08-05
To characterize the basic functions of GPR84 in phagocytes, we have utilized the receptor selective antagonist GLPG1205 (a small selective antagonist of GPR84 developed by Galapagos NV [14]) together with ZQ16 (2-(hexylthio) pyrimidine-4,6-diol), a potent GPR84 selective agonist identified in a high
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Obestatin synthetized mainly in the
2022-08-05
Obestatin, synthetized mainly in the gastrointestinal tract, participates in the regulation of metabolic functioning at both central and peripheral levels (food intake, pancreatic activity or/and adipocytes proliferation) (Granata et al., 2008; Li et al., 2011). It is involved in the complex gut-bra
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Additionally OsGly I overexpressing transgenic rice plants h
2022-08-05
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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It is essential to maintain genome integrity
2022-08-05
It is essential to maintain genome integrity and stability which is assaulted by oxidative stress. To perform this function, all human cells have well developed repair systems. Base excision repair (BER) system is the most effective pathway responsible to revert back lesions caused by oxidative stre
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In addition http www apexbt
2022-08-05
In addition to genomics, transcriptomics and proteomics tools, metabolomics approaches are now used in order to optimize glycoprotein production in CHO cell lines. Recent advances in metabolite quantification have allowed identification of cellular phenotypes under specific experimental conditions (
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Previous studies have suggested that GPR protects from bone
2022-08-05
Previous studies have suggested that GPR40 protects from bone loss via inhibition of osteoclasts. Wittrant et al. used GPR40 knock-out mice and primary osteoclasts to investigate the role of GPR40 on bone remodelling. Their results in primary osteoclast cultures and the RAW264.7 cell line showed tha
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A main finding of this
2022-08-05
A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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The glucocorticoid GR complex exerts wide spread cellular ef
2022-08-05
The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of
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Considering together the conformational docking
2022-08-04
Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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Several small molecules such as erastin and RSL are reported
2022-08-04
Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer ML385 receptor [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-depende
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Literature review suggests a strong presence of
2022-08-04
Literature review suggests a strong presence of central histaminergic transmission in the Dehydrocostus Lactone areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine
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Our results demonstrated that most of the HUA
2022-08-04
Our results demonstrated that most of the HUA rings incubated with 100 μM TBT do not have the capacity to contract in the presence of 5-HT or exhibit very low contractions in comparison to the control. Only 23.3% of the HUA rings were able to contract. These results seem to indicate that there may b
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An azabicyclic compound named S a a hexahydro
2022-08-04
An azabicyclic VEGFR Tyrosine Kinase Inhibitor II receptor named S 38093, (4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide), was introduced by Servier with H3R antagonist and inverse agonist activity (Sors et al., 2017). The compound contains all the drug-likeness criter
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Benzene metabolism occurs primarily in the liver where benze
2022-08-04
Benzene metabolism occurs primarily in the liver where benzene is converted into phenol, catechol, hydroquinone (HQ). HQ is further converted to 1,4-benzoquinone (1,4-BQ) in the bone marrow which is the primary organ of benzene toxicity (Bolton et al., 2000). 1,4-BQ is an important benzene metabolit
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