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On the basis of the findings described above a
2021-07-21
On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed
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Stress is usually comprehended as an event affecting mainly
2021-07-21
Stress is usually comprehended as an event affecting mainly the HPA axis and initiating the alarm reaction represented by activation of the adrenal medulla. This means that the levels of related hormones and neurotransmitters are significantly elevated during and after the stress. CRF, following its
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br Introduction The cys loop ligand gated ion channels
2021-07-21
Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri
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In rodent models the loss of
2021-07-21
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an ll-37 receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthase inhibit
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Hinokitiol has versatile abilities as anticancer antimicrobi
2021-07-21
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 rotenone arrest in many different types of cancers, such as mur
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CM AVM and VOGM are thought to be
2021-07-21
CM-AVM and VOGM are thought to be two distinct disorders, with CM-AVM characterized by atypical CMs, with or without AVM in variable body parts, while VOGM is a type of cerebral AVM [16]. The fact that VOGM is infrequently reported as the AVM in CM-AVM patients, and CMs are quite often identified in
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Several studies have shown that independently of body weight
2021-07-21
Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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In conclusion we have shown that the cellular effects produc
2021-07-20
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC hinokitiol are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high EGFR levels pro
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PBMC derived macrophages not only express
2021-07-20
PBMC-derived macrophages not only express EBI2 but also have the ability to respond to their natural agonist 7α,25-OHC by activating downstream signal transduction pathways. In line with previous findings, our data confirm that receptor stimulation induces calcium mobilization which can be blocked b
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br Funding This work was supported by the grants
2021-07-20
Funding This work was supported by the grants from MSD, Terumo Life Science Foundation, Takeda Science Foundation, and Japan Diabetes Foundation. Disclosures Acknowledgments The authors thank C. Morimoto (Juntendo University, Tokyo, Japan) and K. Takeda (Immunology Frontier Research Center
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As the angular structure of compound
2021-07-20
As the angular structure of compound cannot be differentiated from the linear structure by H NMR spectroscopy, a NOESY NMR experiment was performed to unambiguously characterize the regioselectivity of the final compound. In the linear compound , a signature correlation between the proton of the th
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ack1 inhibitors Members of the Nudix family typically
2021-07-20
Members of the Nudix family typically contain a 23-amino-acid sequence (Nudix box) of GxExREUxEExGU, where U is usually Ile, Leu, or Val and x represents any amino acid. The EUxEE core residues serve as anchors for an Mg ligand that associates with a characteristic pyrophosphate linkage that is comm
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E cadherin is an adhesive Ca dependent
2021-07-20
E-cadherin is an adhesive Ca2+ dependent transmembrane protein mediating tight and strong cell-cell adhesion through homophilic interactions. There is strong evidence in favour of the major role of E-cadherin in melanocytes adhesion to keratinocytes in the LY500307 (Tang et al., 1994). The expressi
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Previous studies reported that NE and
2021-07-20
Previous studies reported that NE and MHPG are deeply involved in depression and that NE reuptake inhibitors are approved for use in patients with depression (for review, see [2]). We found increased hippocampal content of NE and MHPG in the CORT-treated CRTH2−/− mice (Fig. 3). In the hippocampus, a
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As plants can only take
2021-07-20
As plants can only take up P in an inorganic orthophosphate form, it was expected that the proportion of orthophosphate P in the OA would be a good indication of the availability of the P in the OA. While the P speciation of the COMP sample could not be determined by deconvolution due to the broadne
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