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Ung et al examined a variety of structural features
2020-09-27

Ung et al. examined a variety of structural features based upon the location of the DFG-motif and the αC-helix to define the conformational space of the catalytic domain of protein kinases [75]. They reported that the DFG motif can move from its active DFG-Din location to the inactive DFG-Dout locat
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CDK lacks DNA binding domains
2020-09-27

CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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In this study new and more extended tables
2020-09-27

In this study, new and more extended tables of parameters were estimated for pure fluids and binary mixtures that are relevant to biodiesel systems. Also, calculations for glyceride systems will be shown, which is a topic not investigated before with the CPA model. As before [21], [22], [23], [24],
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The intestinal cholesterol absorption markers sitosterol and
2020-09-26

The intestinal cholesterol 5-Methyl-CTP markers sitosterol and campesterol to cholesterol levels were significantly lower in Villin-Tgif1 mice compared to wild type mice, irrespective of diet. However, the decrease was less pronounced in Villin-Tgif1 mice fed a chow diet (∼20–30%) compared to mice
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Hinokitiol has versatile abilities as anticancer antimicrobi
2020-09-25

Hinokitiol has versatile abilities as anticancer, antimicrobial and molecule transport agents and appears to have no developmental toxicity or carcinogenic effects (Imai et al., 2006b). For anticancer activities, it causes apoptosis and G418 arrest in many different types of cancers, such as murine
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br EphB as a therapeutic target
2020-09-25

EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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In bone PGE exerts both anabolic
2020-09-25

In bone, PGE2 exerts both anabolic and catabolic effects [6], [7], [8], [9]. Administration of PGE2 to mice lacking each of the four prostanoid receptors identified EP4 as the primary mediator of PGE2-induced bone formation [10]. While the role of EP1 in osteoblastic differentiation and bone metabol
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The monomeric oligomeric states of DDR
2020-09-25

The monomeric/oligomeric states of DDR2-V5-His and DDR2-Fc were confirmed by Western blotting under reducing and non-reducing conditions. As shown in Fig. 1b, DDR2-V5-His exhibited a relative molecular mass of ~60 kDa under both reducing and non-reducing conditions, consistent with this protein bein
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The important role of miRNAs
2020-09-25

The important role of miRNAs in cellular differentiation has been proposed recently. Previous studies had suggested roles for different miRNAs during osteogenesis [20]. Certain miRNAs could promote osteoblast differentiation, such as miR-194 [20], whereas others could inhibit the cell differentiatio
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Deregulated Wnt signaling either due to pathway mutations or
2020-09-24

Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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The synthetic route of R changed derivatives is shown in
2020-09-24

The synthetic route of R-changed derivatives is shown in . Compounds – were prepared from commercially available 4-nitro-1-indazole (). After same two steps with , the N-substituted indazole of was produced using the Suzuki reaction in a good yield (85%). Reduction of was performed using Pd/C, and t
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In our model CSF R blockade
2020-09-24

In our model, CSF-1R blockade with PLX647 mainly targeted the more abundant MDSCs instead of macrophages, suggesting that the role of CSF-1 may be tumor model-dependent. Different tumor models, genetic backgrounds, or treatments may induce different growth factors or cytokines in the tumor microenv
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Our structures also provide new insights
2020-09-24

Our structures also provide new insights into CRTH2 drug development. The ligand binding pocket revealed by our structures comprises many aromatic residues and a few polar residues at the distal end. Correspondingly, most CRTH2 antagonists share a similar structural feature characterized by an aceta
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hUcn II influence on MAP is mediated by the activation
2020-09-24

hUcn II influence on MAP is mediated by the activation of CRF2 receptors. In vitro binding studies established that hUcn II is a selective ligand for CRF2 receptors with a slightly higher affinities for CRF2β compared with CRF2α and low or no affinity for CRF1 receptor [13], [19], [24]. Recent in vi
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Nicotine is the main psychoactive component of tobacco
2020-09-24

Nicotine is the main psychoactive component of tobacco that causes addiction. Besides the regulation of the stress responses, CRF has been implicated in nicotine addiction based on several lines of evidence (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). First, acute administration of nicotine, l
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