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Previously we have shown that the overexpression
2021-08-16
Previously, we have shown that the overexpression of ERRγ induces exercise-like oxidative muscle remodeling without engaging changes in the expression level or activity of PGC1α (Narkar et al., 2011). In this study, overexpression of ERRγ in PKO muscle reveals that ERRγ-activated target genes can ac
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Given the molecular pharmacology and in vitro
2021-08-16
Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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br Early developments Historically the advent of
2021-08-16
Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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Importantly we observed significantly the reduced
2021-08-16
Importantly, we observed significantly the reduced myocardial infarct size, the improved left ventricular function and the inhibited fibrosis after I/R with oral GA-BH4 supplementation before ischemia (Fig. 1, Fig. 2, Fig. 3). Usually, there is a view that the antioxidation induced by reducing agent
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GNE-317 br Materials and methods br
2021-08-16
Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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Addressing whether impaired activation of D and D receptors
2021-08-16
Addressing whether impaired activation of D1 and D2 receptors regulates memory capacity is relevant for all human pathologies that lead to reduced activation of these ryanodine pathways, such as ageing [39], certain genetic polymorphisms [40] and neurodegenerative disorders. In this study, we have
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Acknowledgments We are grateful to Dr Jean Marie
2021-08-16
Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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Natural and synthetic glucocorticoids perform their biologic
2021-08-14
Natural and synthetic glucocorticoids perform their biological action in the organism through receptor-dependent mechanisms (e.g., by binding to the glucocorticoid receptors). It has been determined that glucocorticoid receptors cross-talk with other nuclear receptors, including AhR (Celander et al.
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Benzoylmesaconitine mg Palliative surgeries for refractory e
2021-08-14
Palliative surgeries for refractory epilepsy include vagus nerve stimulation and corpus callosotomy. Among 220 individuals with CDD with parent-entered data, 17% had a vagus nerve stimulation implanted and 69% of parents reported reduced seizure frequency. These data are consistent with a case repor
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Several lines of evidence suggest
2021-08-14
Several lines of evidence suggest that the anxiety provoking behavioral effects of CRF involve CRF1 receptors. CRF1 knockout mice show increased anxiolytic-like activity in the elevated plus maze and a tendency to enter the illuminated region of a light–dark box [49], [52]. In addition, studies usin
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Several highly selective COX inhibitors coxibs
2021-08-14
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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br Conclusions and future perspectives
2021-08-14
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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br Estrogen receptors activate mGluR signaling pathways
2021-08-14
Estrogen receptors activate mGluR signaling pathways In order to distinguish the opposing effects of estradiol on CREB phosphorylation, we turned to a “bottom-up” approach, working backwards from CREB phosphorylation to pharmacologically isolate the two signaling pathways (Boulware et al., 2005).
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br Conflict of interest br
2021-08-14
Conflict of interest Supplementary methods and materials Acknowledgments This work was supported by an Early Career Researcher grant awarded by the Institute of Health and Biomedical Innovation to IMW and Queensland University of Technology, and grants awarded to SS by the Prostate Cancer F
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cAMP mediated signaling pathways are important
2021-08-14
cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, L-α-Aminoadipic Acid of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased ex
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