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In the preclinical evaluation of CRF
2020-12-01
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Based on both the observational and theoretical data
2020-12-01
Based on both the observational and theoretical data generated in this study, it appears that the mechanism(s) underlying lower IFM CPT1 activity is complex. Modeling enzyme activity versus alterations in catalytic efficiency (Fig. 3A) suggests that the observed age-associated changes in Km and Vmax
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br Functional significance Defects of the lysyl hydroxylases
2020-12-01
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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Since protein kinase CK has over
2020-12-01
Since protein kinase CK2 has over 300 known substrates we examined if the inhibitory effects described above could also be detected using another substrate. Therefore, we employed the synthetic peptide RRRADDSDDDDD which is often used in CK2 inhibitory studies. Quite contrary to the phosphorylation
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The nucleus accumbens is a critical locus for ER
2020-11-30
The nucleus accumbens is a critical locus for ER/mGluR signaling in the context of addiction ER/mGluR signaling is regulated by caveolin proteins and palmitoylation Because of the vast implications of ER/mGluR association, it is important to understand what regulates their interaction. Such regu
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br In addition to the classic nuclear
2020-11-30
In addition to the classic nuclear genomic action, estrogens have been found to induce rapid effects occurring within minutes following administration. These effects are mediated through a subpopulation of estrogen receptors associated with the plasma membrane, a process usually termed “membrane-i
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The mechanism by which OC use
2020-11-30
The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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SS is a high grade malignant soft
2020-11-30
SS is a high-grade malignant soft tissue sarcoma accounting for 5%–10% of soft tissue sarcomas. After RMS, SS is the most common sarcoma in children, adolescents and young adults [9]. SS originates primarily in the lower (62%) and upper (21%) extremities but may occur at any anatomic site [9], [10].
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Given the potency enhancing effect of the butyl
2020-11-30
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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A particularly important system in which Eph ephrin signalin
2020-11-30
A particularly important system in which Eph-ephrin signaling has been widely studied is neural development, in which downstream signal transduction controls neural stem cell (NSC) proliferation, migration, and survival both during early development and in adulthood (19, 20, 21). Furthermore, Eph-ep
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oicr Initial investigations in the heart uncovered
2020-11-30
Initial investigations in the heart uncovered Epac as a positive regulator of myocyte hypertrophy [8], [9]. Concomitantly, Epac has been shown to regulate cardiac Ca homeostasis [8], [10], [11], [12], [13]. Ca is an essential second messenger in the cardiac physiology because its rhythmic variations
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br Disclosures br Acknowledgements This work was supported
2020-11-30
Disclosures Acknowledgements This work was supported by the Natural Science Foundation of China (No. 81560587); the Fok Ying-Tong Education Foundation of China (No. 151107), the basic ability promotion project for young and middle-aged teachers in Universities in Guangxi (No. 2018KY1146) and t
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Enolase as a plasminogen receptor and activator localized on
2020-11-30
Enolase, as a plasminogen receptor and activator localized on the surface of several helminths, can interact with the host fibrinolytic system (Yang et al., 2010, Du et al., 2009, de la Torre-Escudero et al., 2010). The enzyme is also one of excretory/secretory (ES) products in some helminths, such
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To further confirm the roles of the CYP
2020-11-30
To further confirm the roles of the CYP450 enzymes involved in the metabolism of Dip in rat liver microsomes, we utilized not only chemical inhibitors but also a correlation analysis and a panel of recombinant rat CYP450 enzymes to evaluate the contribution of CYP450 enzymes. The results of the corr
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Studies have focused on a hydrophobic
2020-11-30
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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