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This structure guided the variation of the
2021-01-14
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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In addition to PGC transcriptional co repressors
2021-01-14
In addition to PGC1α, transcriptional co-repressors such as NCOR and RIP140 participate in oxidative muscle remodeling induced by exercise, whereby reductions in their expression and the resulting de-repression of downstream TFs activates oxidative gene expression (Seth et al., 2007, Yamamoto et al.
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ATP binding cassette transporters such as
2021-01-14
ATP-binding cassette transporters such as ABCA1 and ABCG1 are expressed on cell membranes to transport cholesterol from Annexin V-Cy3 Apoptosis Kit Plus to HDL. These transporters help to improve RCT and reduce atherosclerosis. ABCA1 and ABCG1 gene expression are primarily induced by the stimulatio
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br Acknowledgments br Introduction Hypertensive retinopathy
2021-01-13
Acknowledgments Introduction Hypertensive retinopathy is a disease of the retinal microvasculature associated with elevated blood pressure (Fraser-Bell et al., 2017). Narrowing of retinal arterioles occurs in the early stage of the disease, and with persistent hypertension further vascular pat
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To determine direct DDR binding partners and
2021-01-13
To determine direct DDR1-binding partners and to further connect to Akt and mTOR signaling, we performed mass spectrometry on DDR1 immunoprecipitates and found various candidates of the Akt and mTOR pathway such as LARP1 (La-related protein 1) and RPS6 (40S ribosomal protein S6/ S6). Most intriguing
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Examination of Wnt signaling via for example
2021-01-13
Examination of Wnt signaling via, for example, complexes of frizzled (Fz) and lipoprotein-receptor-related protein (LRP) receptors has been hindered by difficulties in producing Wnt ligands due to their inherent hydrophobicity [20]. This bottleneck was recently bypassed by constructing highly solubl
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A summary of the drug CDK hydrophobic hydrogen bonding
2021-01-13
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different Camptothecin the same value [77], which facilitates comparisons among differ
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bcrp transporter Signal transduction through IL c
2021-01-13
Signal transduction through IL-34/ c-FMS ligand receptor also leads to the differentiation, survival and, angiogenesis, proliferation, adhesion and migration of cells of the monocyte/macrophage lineage similar to that of CSF-1 through the various pathways-First is through FAK (Focal Adhesion Kinase)
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In the course of our program which was
2021-01-13
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Magnetic interactions between metal ions
2021-01-13
Magnetic interactions between metal ions are usually described by superexchange via intermediate ligands. Although the general principles of the superexchange mechanism are essentially the same for d and f ions, calculations of exchange parameters for lanthanides are more difficult than for transiti
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br Introduction Ewing s sarcoma ES is a
2021-01-13
Introduction Ewing’s sarcoma (ES) is a mesenchymal tumor characterized by small, round, blue cells, and is poorly differentiated and highly malignant [1]. While ES typically arises in bone and soft tissue, rare primary extraosseous manifestations of ES have been reported throughout the body [2].
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Importantly our in vivo data fit to the
2021-01-12
Importantly, our in vivo data fit to the in vitro data, further confirming the synergistic effect of XJD and gefitinib on the inhibition of lung cancer and the regulation of SP1, HOTAIR, and EP4 Dyngo-4a levels. The doses of XJD used were based on our previous in vivo study (Zhao et al., 2016). We b
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The effect of ET activity on the development of
2021-01-12
The effect of ET-1 activity on the development of experimental pulmonary fibrosis has also been examined by other investigators. One study found that repeated administration of Bosentan, an ERA used to treat pulmonary arterial hypertension (PAH), significantly decreased bleomycin-induced pulmonary f
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DAPI hydrochloride br Funding This work was
2021-01-12
Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus
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Bcl functions as a transcription repressor via
2021-01-12
Bcl6 functions as a transcription repressor via its N-terminal BTB domain and middle “second repression,” or “RD2” domain (Chang et al., 1996, Seyfert et al., 1996). A loss of function of the BCL6 BTB domain markedly impairs survival and proliferation of mature GC Octyl-α-ketoglutarate in a B cell
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