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The first GSM was identified from the discovery
2022-09-15
The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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LDE225 Diphosphate br Financial support This work was suppor
2022-09-15
Financial support This work was supported by Fondation pour la Recherche Médicale (Equipe labellisée, DEQ20150331724), Inserm, University of Lille, and Agence Nationale pour la Recherche (ANR-10-LBEX-46 and ANR-10-INBS-08; ProFI project, “Infrastructures Nationales en Biologie et Santé”; “Investi
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The typical pharmacophore for GPR agonists contains four
2022-09-15
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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pyridone In principle an ideal Fenton reaction element
2022-09-15
In principle, an ideal Fenton reaction element should have multiple oxidation states to form a redox cycle in the process of H2O2 decomposition to HO•. Although iron is very effective in catalyzing Fenton reaction, it requires a low pH value (pH 2-4) to reach the optimal catalytic efficiency, which
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Besides its carcinogenic role WTAP was also discovered to
2022-09-15
Besides its carcinogenic role, WTAP was also discovered to participate in several physical processes in normal cells. As previously reported, WTAP was involved in cell proliferation, survival, apoptosis [7,29,30], eye development [8] and embryonic development [7] owing to its complex function in tra
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This SAR work led to the
2022-09-15
This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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Our understanding of the genetic basis of
2022-09-15
Our understanding of the genetic basis of myeloid malignancies has been profoundly improved in recent years. Studies have revealed new recurrent somatic mutations in myeloid malignancies, including myeloproliferative neoplasms (MPNs), myelodysplastic syndrome (MDS) and acute myeloid leukaemia (AML).
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It has been suggested that MAPK Huang et al
2022-09-15
It has been suggested that MAPK (Huang et al., 2013, Uddman et al., 2003, Xu et al., 2008) signaling pathway is involved in the transcriptional upregulation of ETB receptor. The present study demonstrated that treatment with CsA increased phosphorylation of ERK1/2 and p38. Inhibition of ERK1/2 and p
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2449 australia br Materials and methods br Results br Discus
2022-09-15
Materials and methods Results Discussion It has previously been reported that EZH2 plays a key role in the silencing of tumour suppressor genes through methylation of H3K27me3 in the promoter region of these genes in neuroblastoma [32], [40]. In this study, we show that EZH2 is aberrantly g
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Electrochemical techniques have attracted broad attention fo
2022-09-15
Electrochemical techniques have attracted broad attention for their outstanding advantages, such as satisfactory sensitivity and convenient operation. Nowadays, nucleic PKC412 nanostructures such as DNA tetrahedron structure, nucleic acid-mimicking structure, exhibit noticeable application in the f
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br Introduction Histamine stored in
2022-09-15
Introduction Histamine stored in mast cells and basophils has been recognized as one of the most critical mediators in allergic reactions and plays an important role in eliciting the nasal symptoms of allergic rhinitis, such as sneezing, nasal itch, pain, rhinorrhea, and congestion [1], [2]. It i
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br ABT aR aR methyl hexahydropyrrolo b
2022-09-15
ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo
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Waldeck Weiermair et al demonstrated that in endothelial cel
2022-09-09
Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp
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P gps expressed in cells and
2022-09-09
P-gps, expressed in nefiracetam and tissues of human and animals, play an active role in cellular protection against multiple toxicants by transporting them out of a cell. Thus, improving transport activity of P-gp may contribute to removing Cd from living oysters. Cd accumulation in the cultured c
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Although the overall structures of mGlu
2022-09-09
Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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